The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
Synthetic reagent and applications OF ALUMINIUM ISOPROPOXIDEShikha Popali
SYNTHETIC REAGENTS AND APPLICATIONS OF ALUMINIUM ISOPROPOXIDE ITS ALTERNATIVE NAMES AND ITS PHYSICAL PROPERTIRS , HANDLING, STORAGE, PRECAUTIONS, PREPARATIONS, SYNTHETIC APPLICATIONS
Mitsunubu reaction had been synthesised by Japanese scientist OYO Mitsunbu.
It involves the Conversion of primary, Secondary alcohol into the ester group.
It follows SN2 mechanism.
Dakin reaction- organic and Heterocyclic chemistry- As per PCI syllabusAkhil Nagar
The Dakin reaction involves the replacement of an aldehyde group on ortho and para hydroxy and ortho amino-benzaldehyde (or ketone) compounds with a hydroxyl group when reacted with alkaline hydrogen peroxide. The mechanism involves the aldehyde group being oxidized by hydrogen peroxide to a carboxyl group, which then undergoes base hydrolysis to form the hydroxyl substituted product.
The document discusses the indole molecule, including its structure, biological activities, and importance in pharmaceuticals. It provides examples of many indole-containing drugs and toxins. Synthetic routes for producing indoles are also covered, such as the Fischer indole synthesis and methods involving phenylhydrazones, diazonium salts, and propargyl alcohols. The indole nucleus is an important scaffold in natural products and drugs.
The Perkin reaction is an organic reaction that produces α,β-unsaturated aromatic acids by condensing an aromatic aldehyde with an aliphatic acid anhydride in the presence of a weak base. The reaction was first discovered by William Henry Perkin in 1868. It involves the removal of water through condensation and produces the desired unsaturated carboxylic acid. Some examples of the Perkin reaction include converting furfural to furylacrylic acid, forming coumaric acid from salicylaldehyde which can then be dehydrated to coumarin, and synthesizing the phytoestrogenic compound resveratrol.
The Birch reduction is a reaction where aromatic compounds undergo partial reduction to unconjugated cyclohexadiene compounds in the presence of alkali metals like sodium or lithium in liquid ammonia. The solvated electrons from the reaction of the metal with liquid ammonia give the solution an intense blue color. The mechanism begins with single electron transfer from the metal to the aromatic ring, forming a radical anion. Regioselectivity in the reduction depends on whether substituents on the aromatic ring are electron donating groups or electron withdrawing groups. The Birch reduction can selectively reduce the less electron-rich ring in bicyclic aromatic compounds.
Asymmetric synthesis FOR BSc, MSc, Bpharm, M,pharmShikha Popali
This document discusses different methods for asymmetric synthesis, which is the production of a single enantiomer from an achiral starting material. It describes chiral pool synthesis, which uses naturally occurring chiral compounds as starting materials. It also explains chiral auxiliaries, where an enantiopure auxiliary is attached and later removed, leaving the desired enantiomer. Chiral reagents and chiral catalysts are also discussed, where an enantiopure reagent or catalyst leads to an enantioselective reaction. Specific examples include the use of chiral boron hydrides and ligands like BINAP. Asymmetric hydrogenation is given as another key method. The document emphasizes the importance of these techniques for drug safety and mimicking nature.
Synthetic reagent and applications OF ALUMINIUM ISOPROPOXIDEShikha Popali
SYNTHETIC REAGENTS AND APPLICATIONS OF ALUMINIUM ISOPROPOXIDE ITS ALTERNATIVE NAMES AND ITS PHYSICAL PROPERTIRS , HANDLING, STORAGE, PRECAUTIONS, PREPARATIONS, SYNTHETIC APPLICATIONS
Mitsunubu reaction had been synthesised by Japanese scientist OYO Mitsunbu.
It involves the Conversion of primary, Secondary alcohol into the ester group.
It follows SN2 mechanism.
Dakin reaction- organic and Heterocyclic chemistry- As per PCI syllabusAkhil Nagar
The Dakin reaction involves the replacement of an aldehyde group on ortho and para hydroxy and ortho amino-benzaldehyde (or ketone) compounds with a hydroxyl group when reacted with alkaline hydrogen peroxide. The mechanism involves the aldehyde group being oxidized by hydrogen peroxide to a carboxyl group, which then undergoes base hydrolysis to form the hydroxyl substituted product.
The document discusses the indole molecule, including its structure, biological activities, and importance in pharmaceuticals. It provides examples of many indole-containing drugs and toxins. Synthetic routes for producing indoles are also covered, such as the Fischer indole synthesis and methods involving phenylhydrazones, diazonium salts, and propargyl alcohols. The indole nucleus is an important scaffold in natural products and drugs.
The Perkin reaction is an organic reaction that produces α,β-unsaturated aromatic acids by condensing an aromatic aldehyde with an aliphatic acid anhydride in the presence of a weak base. The reaction was first discovered by William Henry Perkin in 1868. It involves the removal of water through condensation and produces the desired unsaturated carboxylic acid. Some examples of the Perkin reaction include converting furfural to furylacrylic acid, forming coumaric acid from salicylaldehyde which can then be dehydrated to coumarin, and synthesizing the phytoestrogenic compound resveratrol.
The Birch reduction is a reaction where aromatic compounds undergo partial reduction to unconjugated cyclohexadiene compounds in the presence of alkali metals like sodium or lithium in liquid ammonia. The solvated electrons from the reaction of the metal with liquid ammonia give the solution an intense blue color. The mechanism begins with single electron transfer from the metal to the aromatic ring, forming a radical anion. Regioselectivity in the reduction depends on whether substituents on the aromatic ring are electron donating groups or electron withdrawing groups. The Birch reduction can selectively reduce the less electron-rich ring in bicyclic aromatic compounds.
Asymmetric synthesis FOR BSc, MSc, Bpharm, M,pharmShikha Popali
This document discusses different methods for asymmetric synthesis, which is the production of a single enantiomer from an achiral starting material. It describes chiral pool synthesis, which uses naturally occurring chiral compounds as starting materials. It also explains chiral auxiliaries, where an enantiopure auxiliary is attached and later removed, leaving the desired enantiomer. Chiral reagents and chiral catalysts are also discussed, where an enantiopure reagent or catalyst leads to an enantioselective reaction. Specific examples include the use of chiral boron hydrides and ligands like BINAP. Asymmetric hydrogenation is given as another key method. The document emphasizes the importance of these techniques for drug safety and mimicking nature.
The Schmidt reaction is an organic reaction in which an azide reacts with a carbonyl derivative, usually a aldehyde, ketone, or carboxylic acid, under acidic conditions to give an amine or amide, with expulsion of nitrogen
Quinoline is a heterocyclic aromatic organic compound with the chemical formula C9H7N. It is a heterocyclic analogue of naphthalene that can be obtained by fusing a benzene ring to a pyridine nucleus. Quinoline and its derivatives have various medicinal uses, including as antimalarials, amebicides, treatments for infections caused by bacteria such as pneumonia and gonorrhea, and as a chemotherapeutic agent for treating leukemia.
Indole is an aromatic heterocyclic organic compound. It contains a benzene ring fused to a pyrrole ring. Indole occurs naturally in human feces and has an intense fecal odor. It is also found in coal tar and contributes to the scents of many flowers. Electrophilic aromatic substitution of indole occurs preferentially on the five-membered pyrrole ring. Indole can be synthesized via Fischer indole synthesis or Leimgruber synthesis. It has several pharmaceutical and medical uses including for treating cancer, fibromyalgia, and schizophrenia.
The document discusses several heterocyclic compounds including quinolines, isoquinolines, and indoles. It summarizes key reactions used to synthesize these compounds, including the Combes, Friedlander, Knorr, and Skraup reactions for quinoline synthesis. It also discusses the Bischler-Napieralski, Pictet-Spengler, and Pomeranz-Fritsch reactions for isoquinoline synthesis and the Fischer, Madelung, and Reissert reactions for indole synthesis, along with mechanisms and examples of each reaction. Reactivity and substitution patterns are also covered for quinolines, isoquinolines and indoles.
Clemmensen reduction- Heterocyclic and Organic chemistry- As per PCI syllabusAkhil Nagar
The Clemmensen reduction allows the deoxygenation of aldehydes or ketones using zinc amalgam and hydrochloric acid. This converts the carbonyl group to a methylene group, producing the corresponding hydrocarbon. It is useful for substrates that are stable to strong acid, as the acidic conditions would degrade acid-labile molecules. The mechanism involves zinc carbenoids as intermediates in the reduction, without requiring alcohol intermediates. Zinc amalgam is an alloy of zinc and mercury that dissolves zinc smoothly and evenly in the reaction mixture to facilitate the reduction.
The Beckmann rearrangement is an acid-catalyzed reaction that converts ketoximes to amides. It was discovered by German chemist Ernst Otto Beckmann in the late 19th century. This rearrangement can occur in both cyclic and acyclic compounds, converting ketoximes to lactams or amides, respectively. Common reagents used to catalyze the Beckmann rearrangement include concentrated sulfuric acid, hydrochloric acid, and phosphorus pentachloride. The reaction proceeds through the formation of a nitrilium ion intermediate followed by hydrolysis to form the final amide product. The Beckmann rearrangement has applications in synthesizing drugs like paracetamol and polymers like nylon.
1. Quinoline is a heterocyclic aromatic organic compound with the chemical formula C9H7N. It is colorless and hygroscopic, becoming yellow and brown over time when exposed to light.
2. Quinoline itself has few applications but many derivatives are useful, including quinine which is an important anti-malarial drug. Over 200 biologically active quinoline alkaloids have been identified.
3. The document discusses the structure, properties, synthesis methods like Skraup, Doebner-Miller, and Conrad-Limpach, reactions including electrophilic substitution, oxidation, and reduction, and applications of quinoline and its derivatives in dyes
The document summarizes the Biginelli reaction, which was discovered in 1893 by Italian chemist Pietro Biginelli. It involves the acid-catalyzed cyclocondensation of beta-keto esters, aldehydes, and urea or thiourea in alcohols to produce dihydropyrimidinones (DHPMs). DHPMs have potential pharmaceutical applications and several exhibit biological activities. The document discusses the reaction mechanism, recent advances like asymmetric synthesis and solid-phase approaches, and applications of DHPMs such as in pharmacology and natural product synthesis.
This document discusses several reagents used in organic synthesis:
1) Wittig reagent is used to synthesize alkenes from ketones and aldehydes via the Wittig reaction. It is prepared from triphenylphosphine and alkyl halides.
2) Diazopropane is used for cyclopropanation of alkenes and is prepared by oxidation of acetohydrazone.
3) BOP reagent is commonly used for peptide coupling and esterification due to its ability to form reactive hydroxybenzotriazolyl intermediates. It involves generation of a carboxylate anion which attacks the phosphorus center.
Purines are the cyclic diureides, consisting of a pyrimidine ring fused with an imidazole ring. Purine m.p. 212-213⁰C is a synthetic compound. Purine is not found naturally, but it’s derivatives, adenine, and guanine are found in nature. These are the building blocks of nucleic acid RNA and DNA. Purine can exist in four tautomeric forms in which the hydrogen atom is attached to the different nitrogen atom, N-1, N-3, N-7, and N-9. Purines are a type of chemical compound found in foods and drinks that are part of a normal diet. A small number of foods contain concentrated levels of purines, such as seafood, organ meats, and alcoholic beverages, especially beer.
The document summarizes two organic reactions: the Dieckmann reaction and ozonolysis reaction. The Dieckmann reaction involves the intramolecular condensation of diesters in the presence of a strong base to form β-keto esters via a 5-exo-trig cyclization. It is used to synthesize cyclopentane and cyclohexane derivatives. Ozonolysis involves the cleavage of unsaturated bonds like alkenes and alkynes with ozone to form carbonyl groups. It can be used to oxidize alkenes into alcohols, aldehydes, ketones or carboxylic acids and is useful for structure elucidation of unknown compounds containing carbon-carbon double bonds.
This document summarizes the rearrangement of benzilic acid from benzil. It introduces benzilic acid and notes that it can be prepared through rearrangement of the 1,2-α-diketone benzil. The document then outlines the preparation of benzil, the rearrangement mechanism involving nucleophilic addition and migration, and properties of the resulting benzilic acid including its white crystalline structure and solubility in alcohols. Hazards of benzilic acid are also mentioned, noting it is very hazardous if in contact with skin or eyes or if ingested or inhaled, and that it is chemically stable under recommended storage conditions.
The document summarizes the Baylis-Hillman reaction, which is a carbon-carbon bond forming reaction between an activated alkene and an aldehyde or carbon electrophile catalyzed by a nucleophilic catalyst. The reaction produces densely functionalized products. Key advantages of the reaction include its atom economy, ability to generate chiral centers for asymmetric synthesis, and potential for further functionalization of products. Examples are given of the reaction being used in the synthesis of drugs such as pregabalin and sampatrilat. Mechanisms and strategies to improve the reaction are also discussed.
The Ullmann reaction involves the condensation of aryl halides in the presence of finely divided copper or copper bronze at an elevated temperature to form diaryl derivatives. Two proposed mechanisms are the free radical mechanism, where copper generates an aryl radical, and the ionic mechanism, where an organocuprate intermediate is formed. The Ullmann reaction is useful for synthesizing biaryls, polyaryls, diaryl amines, diaryl ethers, and gossypol.
This powerpoint is about the swern oxidation...It is used for the oxidaton of alcohol and inorder to avoid the chromium reagent. Follow me through youtube
CHE-MYSTERY
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This document discusses heterocyclic compounds called diazines. It describes the three main types of diazines - pyridazine, pyrimidine, and pyrazine. It discusses their properties, including being stable, colorless compounds that are soluble in water. It then covers several common methods for synthesizing each type of diazine, such as using dicarbonyl compounds and hydrazines for pyridazines or dicarbonyls and diamines for pyrazines. The document concludes by covering some notable syntheses of specific diazines and their uses, as well as various reactions diazines undergo, such as reactions with oxidizing agents, nucleophilic reagents, and radicals.
This document discusses heterocyclic compounds, specifically pyrazoles. It describes pyrazoles as a 5-membered heterocyclic ring containing two nitrogen atoms at the 1st and 2nd positions. Several common synthesis routes for pyrazoles are outlined, including the Paal-Knorr synthesis using 1,3-dicarbonyl compounds and hydrazines. The document also reviews reactions that pyrazoles undergo, such as electrophilic substitution, oxidation, and reduction. Finally, some medicinal uses of pyrazoles are provided, including their use as anti-pyretic, analgesic, and anti-inflammatory drugs.
Synthon or Disconnection or Retrosynthesis Approach in Organic Synthesis. This document discusses the key concepts and approaches of retrosynthesis including: 1) Disconnecting a target molecule into logical fragments through breaking bonds to obtain starting materials, 2) It is the reverse of chemical synthesis, 3) Terminologies such as disconnection, synthon, and reagents, 4) Basic rules for preferred disconnections.
Sulfonic acid functionalized silica a remarkably efficient heterogeneous reus...Alexander Decker
This document summarizes research on using a sulfonic acid-functionalized silica catalyst for one-pot multi-component synthesis of amidoalkyl naphthols. Key points:
- The catalyst allows high-yielding synthesis of amidoalkyl naphthols from aryl aldehydes, 2-naphthol, and acetonitrile or amide under solvent-free thermal conditions.
- The catalyst is easily prepared, stable up to 300°C, reusable without loss of activity, and efficient under reaction conditions.
- The method has advantages of being cleaner, simpler, and more environmentally friendly compared to other catalysts due to shorter reaction times, non-toxic reagents, and
This document describes a one-pot method for synthesizing quinoxalines from vicinal diols and keto alcohols with diamines using a gold-carbon nanotube nanohybrid catalyst. The reaction involves an oxidation-condensation cascade where the vicinal diols and keto alcohols are first oxidized to the corresponding diketones or ketones under mild conditions, and these products then condense in situ with aromatic diamines to form various substituted quinoxalines in excellent yields of 87-96% within 26-40 hours. The gold-carbon nanotube nanohybrid catalyst provides high activity, recyclability, and heterogeneous catalysis
The Schmidt reaction is an organic reaction in which an azide reacts with a carbonyl derivative, usually a aldehyde, ketone, or carboxylic acid, under acidic conditions to give an amine or amide, with expulsion of nitrogen
Quinoline is a heterocyclic aromatic organic compound with the chemical formula C9H7N. It is a heterocyclic analogue of naphthalene that can be obtained by fusing a benzene ring to a pyridine nucleus. Quinoline and its derivatives have various medicinal uses, including as antimalarials, amebicides, treatments for infections caused by bacteria such as pneumonia and gonorrhea, and as a chemotherapeutic agent for treating leukemia.
Indole is an aromatic heterocyclic organic compound. It contains a benzene ring fused to a pyrrole ring. Indole occurs naturally in human feces and has an intense fecal odor. It is also found in coal tar and contributes to the scents of many flowers. Electrophilic aromatic substitution of indole occurs preferentially on the five-membered pyrrole ring. Indole can be synthesized via Fischer indole synthesis or Leimgruber synthesis. It has several pharmaceutical and medical uses including for treating cancer, fibromyalgia, and schizophrenia.
The document discusses several heterocyclic compounds including quinolines, isoquinolines, and indoles. It summarizes key reactions used to synthesize these compounds, including the Combes, Friedlander, Knorr, and Skraup reactions for quinoline synthesis. It also discusses the Bischler-Napieralski, Pictet-Spengler, and Pomeranz-Fritsch reactions for isoquinoline synthesis and the Fischer, Madelung, and Reissert reactions for indole synthesis, along with mechanisms and examples of each reaction. Reactivity and substitution patterns are also covered for quinolines, isoquinolines and indoles.
Clemmensen reduction- Heterocyclic and Organic chemistry- As per PCI syllabusAkhil Nagar
The Clemmensen reduction allows the deoxygenation of aldehydes or ketones using zinc amalgam and hydrochloric acid. This converts the carbonyl group to a methylene group, producing the corresponding hydrocarbon. It is useful for substrates that are stable to strong acid, as the acidic conditions would degrade acid-labile molecules. The mechanism involves zinc carbenoids as intermediates in the reduction, without requiring alcohol intermediates. Zinc amalgam is an alloy of zinc and mercury that dissolves zinc smoothly and evenly in the reaction mixture to facilitate the reduction.
The Beckmann rearrangement is an acid-catalyzed reaction that converts ketoximes to amides. It was discovered by German chemist Ernst Otto Beckmann in the late 19th century. This rearrangement can occur in both cyclic and acyclic compounds, converting ketoximes to lactams or amides, respectively. Common reagents used to catalyze the Beckmann rearrangement include concentrated sulfuric acid, hydrochloric acid, and phosphorus pentachloride. The reaction proceeds through the formation of a nitrilium ion intermediate followed by hydrolysis to form the final amide product. The Beckmann rearrangement has applications in synthesizing drugs like paracetamol and polymers like nylon.
1. Quinoline is a heterocyclic aromatic organic compound with the chemical formula C9H7N. It is colorless and hygroscopic, becoming yellow and brown over time when exposed to light.
2. Quinoline itself has few applications but many derivatives are useful, including quinine which is an important anti-malarial drug. Over 200 biologically active quinoline alkaloids have been identified.
3. The document discusses the structure, properties, synthesis methods like Skraup, Doebner-Miller, and Conrad-Limpach, reactions including electrophilic substitution, oxidation, and reduction, and applications of quinoline and its derivatives in dyes
The document summarizes the Biginelli reaction, which was discovered in 1893 by Italian chemist Pietro Biginelli. It involves the acid-catalyzed cyclocondensation of beta-keto esters, aldehydes, and urea or thiourea in alcohols to produce dihydropyrimidinones (DHPMs). DHPMs have potential pharmaceutical applications and several exhibit biological activities. The document discusses the reaction mechanism, recent advances like asymmetric synthesis and solid-phase approaches, and applications of DHPMs such as in pharmacology and natural product synthesis.
This document discusses several reagents used in organic synthesis:
1) Wittig reagent is used to synthesize alkenes from ketones and aldehydes via the Wittig reaction. It is prepared from triphenylphosphine and alkyl halides.
2) Diazopropane is used for cyclopropanation of alkenes and is prepared by oxidation of acetohydrazone.
3) BOP reagent is commonly used for peptide coupling and esterification due to its ability to form reactive hydroxybenzotriazolyl intermediates. It involves generation of a carboxylate anion which attacks the phosphorus center.
Purines are the cyclic diureides, consisting of a pyrimidine ring fused with an imidazole ring. Purine m.p. 212-213⁰C is a synthetic compound. Purine is not found naturally, but it’s derivatives, adenine, and guanine are found in nature. These are the building blocks of nucleic acid RNA and DNA. Purine can exist in four tautomeric forms in which the hydrogen atom is attached to the different nitrogen atom, N-1, N-3, N-7, and N-9. Purines are a type of chemical compound found in foods and drinks that are part of a normal diet. A small number of foods contain concentrated levels of purines, such as seafood, organ meats, and alcoholic beverages, especially beer.
The document summarizes two organic reactions: the Dieckmann reaction and ozonolysis reaction. The Dieckmann reaction involves the intramolecular condensation of diesters in the presence of a strong base to form β-keto esters via a 5-exo-trig cyclization. It is used to synthesize cyclopentane and cyclohexane derivatives. Ozonolysis involves the cleavage of unsaturated bonds like alkenes and alkynes with ozone to form carbonyl groups. It can be used to oxidize alkenes into alcohols, aldehydes, ketones or carboxylic acids and is useful for structure elucidation of unknown compounds containing carbon-carbon double bonds.
This document summarizes the rearrangement of benzilic acid from benzil. It introduces benzilic acid and notes that it can be prepared through rearrangement of the 1,2-α-diketone benzil. The document then outlines the preparation of benzil, the rearrangement mechanism involving nucleophilic addition and migration, and properties of the resulting benzilic acid including its white crystalline structure and solubility in alcohols. Hazards of benzilic acid are also mentioned, noting it is very hazardous if in contact with skin or eyes or if ingested or inhaled, and that it is chemically stable under recommended storage conditions.
The document summarizes the Baylis-Hillman reaction, which is a carbon-carbon bond forming reaction between an activated alkene and an aldehyde or carbon electrophile catalyzed by a nucleophilic catalyst. The reaction produces densely functionalized products. Key advantages of the reaction include its atom economy, ability to generate chiral centers for asymmetric synthesis, and potential for further functionalization of products. Examples are given of the reaction being used in the synthesis of drugs such as pregabalin and sampatrilat. Mechanisms and strategies to improve the reaction are also discussed.
The Ullmann reaction involves the condensation of aryl halides in the presence of finely divided copper or copper bronze at an elevated temperature to form diaryl derivatives. Two proposed mechanisms are the free radical mechanism, where copper generates an aryl radical, and the ionic mechanism, where an organocuprate intermediate is formed. The Ullmann reaction is useful for synthesizing biaryls, polyaryls, diaryl amines, diaryl ethers, and gossypol.
This powerpoint is about the swern oxidation...It is used for the oxidaton of alcohol and inorder to avoid the chromium reagent. Follow me through youtube
CHE-MYSTERY
Subscribe and press bell button for notfcation
This document discusses heterocyclic compounds called diazines. It describes the three main types of diazines - pyridazine, pyrimidine, and pyrazine. It discusses their properties, including being stable, colorless compounds that are soluble in water. It then covers several common methods for synthesizing each type of diazine, such as using dicarbonyl compounds and hydrazines for pyridazines or dicarbonyls and diamines for pyrazines. The document concludes by covering some notable syntheses of specific diazines and their uses, as well as various reactions diazines undergo, such as reactions with oxidizing agents, nucleophilic reagents, and radicals.
This document discusses heterocyclic compounds, specifically pyrazoles. It describes pyrazoles as a 5-membered heterocyclic ring containing two nitrogen atoms at the 1st and 2nd positions. Several common synthesis routes for pyrazoles are outlined, including the Paal-Knorr synthesis using 1,3-dicarbonyl compounds and hydrazines. The document also reviews reactions that pyrazoles undergo, such as electrophilic substitution, oxidation, and reduction. Finally, some medicinal uses of pyrazoles are provided, including their use as anti-pyretic, analgesic, and anti-inflammatory drugs.
Synthon or Disconnection or Retrosynthesis Approach in Organic Synthesis. This document discusses the key concepts and approaches of retrosynthesis including: 1) Disconnecting a target molecule into logical fragments through breaking bonds to obtain starting materials, 2) It is the reverse of chemical synthesis, 3) Terminologies such as disconnection, synthon, and reagents, 4) Basic rules for preferred disconnections.
Sulfonic acid functionalized silica a remarkably efficient heterogeneous reus...Alexander Decker
This document summarizes research on using a sulfonic acid-functionalized silica catalyst for one-pot multi-component synthesis of amidoalkyl naphthols. Key points:
- The catalyst allows high-yielding synthesis of amidoalkyl naphthols from aryl aldehydes, 2-naphthol, and acetonitrile or amide under solvent-free thermal conditions.
- The catalyst is easily prepared, stable up to 300°C, reusable without loss of activity, and efficient under reaction conditions.
- The method has advantages of being cleaner, simpler, and more environmentally friendly compared to other catalysts due to shorter reaction times, non-toxic reagents, and
This document describes a one-pot method for synthesizing quinoxalines from vicinal diols and keto alcohols with diamines using a gold-carbon nanotube nanohybrid catalyst. The reaction involves an oxidation-condensation cascade where the vicinal diols and keto alcohols are first oxidized to the corresponding diketones or ketones under mild conditions, and these products then condense in situ with aromatic diamines to form various substituted quinoxalines in excellent yields of 87-96% within 26-40 hours. The gold-carbon nanotube nanohybrid catalyst provides high activity, recyclability, and heterogeneous catalysis
1) A new reaction is reported that uses ethylene-1,2-diamines or o-phenylenediamines, aromatic aldehydes, and TMSCN to provide a straightforward route to synthesize 2-aminopyrazines and 2-aminoquinoxalines.
2) DBU is found to be a superior promoter of this reaction, accelerating the rate and providing good yields. The reaction involves desilylation, Strecker reaction, amidine-forming cyclization, and dehydrogenative aromatization in a tandem sequence.
3) The reaction scope is investigated and found to work for a variety of aromatic aldehydes containing electron-withdrawing and electron
1) Self-assembled monolayer coated gold nanoparticles catalyze the aerobic oxidation of alpha-hydroxy ketones to aryl 1,2-diketones in water.
2) This provides an efficient one-pot synthesis of quinoxaline derivatives by in situ oxidation of alpha-hydroxy ketones and subsequent condensation with aryl 1,2-diamines in water.
3) 4-Aminothiophenol self-assembled monolayer coated gold nanoparticles were found to be an effective catalyst for these reactions, providing good to excellent yields of products under mild conditions in water.
Synthesis of 1,5 Benzodiazepines A ReviewYogeshIJTSRD
Benzodiazepines are bicyclic heterocycles having medicinal importance. As a result several greener procedures have been developed using mild conditions and recyclable catalysts, easy work up good yields, multi component reactions less wastage and solvent less synthesis. Deepali Mahajan | Abhishek Raina "Synthesis of 1,5- Benzodiazepines: A Review" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-5 | Issue-5 , August 2021, URL: https://www.ijtsrd.com/papers/ijtsrd43842.pdf Paper URL: https://www.ijtsrd.com/chemistry/other/43842/synthesis-of-15-benzodiazepines-a-review/deepali-mahajan
Synthesis And Characterization of Novel Processable Poly (EtherAzomethine)S C...inventionjournals
The novel dialdehyde 1,1-bis[4-(4-benzaldehyde oxy) phenyl] cyclopentane (III) (BBPC) was synthesized starting from cyclopentanone and phenol to give 1, 1-Bis (4-hydroxy phenyl) cyclopentane (II); followed by reaction with p- fluorobenzaldehyde in N, N-dimethyl formamide (DMAc), containing anhydrous potassium carbonate. New series of poly (ether – azomethine)s were synthesized from (BBPC) with different diamines such as 4, 4’- diamino diphenyl ether (ODA),4,4’-diaminodiphenyl methane(MDA),4-aminophenyl sulfone(SDA), p-phenylene diamines, etc. in DMAc with 5 wt% LiCl by solution polycondensation technique. Inherent viscosities of these polymers were in the range 0.19 to 0.42 dL/g indicating formation of moderate molecular weights. These polymers exhibited good solubility in various polar aprotic solvents such as Nmethylpyrrolidone (NMP), N, N-dimethylacetamide (DMAc) and N,N-dimethyl formamide (DMF), etc. X-Ray diffraction pattern of polymers showed that introduction of cardo cyclopentylidene moiety containing ether linkage would disrupt the chain regularity and packing, leading to amorphous nature. Thermal analysis by TGA showed excellent thermal stability of polymers. The structure- property correlation among these polyazomethines were studied; in view of their potential applications as high performance polymers.
This document describes a study that developed an efficient method for synthesizing 2-amino-3-cyano-4H-pyran derivatives using a three-component reaction. The reaction involves the cyclocondensation of aldehydes, malononitrile, and ethyl acetoacetate using ammonium hydroxide as a catalyst under infrared irradiation. The method offers high yields, short reaction times of 10 minutes, and does not require hazardous reagents or conditions. Various substituted aromatic, heteroaromatic, and aliphatic aldehydes successfully provided the desired pyran products in good to excellent yields. The reaction mechanism is proposed to occur through initial Knoevenagel condensation and subsequent Michael addition and cyclization
Copper catalyzed synthesis of N-Heterocycles containing one M-atomssusercbfc01
This document summarizes copper-catalyzed methods for synthesizing various N-heterocycles containing one nitrogen atom. It discusses the synthesis of pyrrole, pyrrolidine, indole, and indolone derivatives using copper catalysts under mild conditions. Various studies are reviewed that achieve these syntheses with good yields and functional group tolerance. Copper catalysts offer advantages over other metals like palladium in providing cost-effective routes for producing valuable pharmaceutical compounds. Future work may focus on developing more sustainable and efficient copper-catalyzed methods.
Antioxident Activity of Greenly Synthesized Anhydrideijtsrd
One pot synthesis of acid esters by Stobbe condensation of alkylidene / arylidene succinates and aldehydes or ketones, their subsequent hydrolysis to diacids hasreported. TheStobbe condensation of various aromatic aldehydes or ketones with dimethyl succinate gives different types of cyclized productsthrough green approach. The improved yields of Fulgenic acid and its anhydridehave observed by the green approach method as compared with other classical methods employed so far.The antioxidant activity of anhydride compounds have done by using DPPH. Yadav Hanuman Singh | Gani Saba"Antioxident Activity of Greenly Synthesized Anhydride" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-2 | Issue-1 , December 2017, URL: http://www.ijtsrd.com/papers/ijtsrd5847.pdf http://www.ijtsrd.com/chemistry/other/5847/antioxident-activity-of-greenly-synthesized-anhydride/yadav-hanuman-singh
Synthesis and Characterization of cyclohexylidene containing novel cardo pol...inventionjournals
International Journal of Engineering and Science Invention (IJESI) is an international journal intended for professionals and researchers in all fields of computer science and electronics. IJESI publishes research articles and reviews within the whole field Engineering Science and Technology, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
A green synthesis of isatoic anhydrides from isatins with urea–hydrogen perox...fer18400
The document describes a green synthesis method for producing isatoic anhydrides from isatins using urea-hydrogen peroxide complex and ultrasound irradiation. Four reaction procedures were tested using urea-hydrogen peroxide as the oxidizing agent and sulfuric acid as a catalyst. The procedures used either acetic anhydride/acetic acid or formic acid as solvents. Ultrasound irradiation was found to dramatically reduce reaction times from 2-24 hours down to 20-135 minutes. The method provides isatoic anhydrides in good yields and with high purity under mild conditions. Combining formic acid and ultrasound yielded the best results for most isatins tested.
The document discusses coumarins, which are naturally occurring compounds with diverse pharmacological properties. Coumarins are found in many plant species and have a wide range of biological activities. Some examples mentioned include uses as anticoagulants, antimicrobials, anti-inflammatories, and more. Common coumarin derivatives discussed include warfarin and various synthetic routes for producing coumarins are also summarized such as the Perkin reaction and Pechmann condensation.
Novel coumarin isoxazoline derivatives: Synthesis and study of antibacterial ...Ratnakaram Venkata Nadh
A highly efficient and mild protocol for the syntheses of ethyl-3-
[7-benzyloxy-4-methyl-2-oxo-2H-8-chromenyl]-5-aryl-4,5-dihydro-4-
isoxazole carboxylates and ethyl-3-[7-benzyloxy-3-chloro-4-methyl-2-
oxo-2H-8-chromenyl]-5-aryl-4,5-dihydro-4-isoxazole carboxylates in
good yields via [3 þ 2] cycloaddition of in situ–generated nitrile
oxides from 7-benzyloxy-4-methyl-coumarin hydroxymoylchlorides
and 7-benzyloxy-3-chloro-4-methyl-coumarin hydroxymoylchlorides
respectively with ethyl-3-aryl prop-2-enoate has been developed.
The new compounds are screened for antibacterial activity.
PEGylated magnetic nanoparticles (PEG@Fe3O4) as cost effectivealternative for...Pawan Kumar
An efficient, cost effective and environmental friendly PEGylated magnetic nanoparticle catalyzed oxida-tive cyanation via CH activation of tertiary amines to corresponding -aminonitriles using hydrogenperoxide as oxidant and sodium cyanide as cyanide source is described. The synthesized nanocatalyst waseasily recovered with the help of external magnet and was successfully reused for several runs withoutany significant loss in catalytic activity.
PEGylated magnetic nanoparticles (PEG@Fe3O4) as cost effectivealternative for...Pawan Kumar
tAn efficient, cost effective and environmental friendly PEGylated magnetic nanoparticle catalyzed oxida-tive cyanation via CH activation of tertiary amines to corresponding -aminonitriles using hydrogenperoxide as oxidant and sodium cyanide as cyanide source is described. The synthesized nanocatalyst waseasily recovered with the help of external magnet and was successfully reused for several runs withoutany significant loss in catalytic activity.
The document provides information about quinoline, isoquinoline, and indole. It discusses their structures, properties, synthesis methods, and reactions. Quinoline and isoquinoline are both heterocyclic aromatic compounds composed of a benzene ring fused to a pyridine ring. They undergo similar electrophilic and nucleophilic substitution reactions. Common synthesis routes for quinoline include the Skraup, Doebner-Miller, and Conrad-Limpach reactions. Isoquinoline synthesis methods include the Pomeranz-Fritsch and Bischler-Napieralski reactions. Indole is a bicyclic molecule with a benzene and pyrrole ring. It does not readily
This document is a project report for an M.Sc. in Chemistry. The project involved synthesizing various functional heterocyclic compounds using a simple, eco-friendly, and cost-effective method with PEG-400 as the solvent. The report details the hypothesis, procedure, results, and schemes for synthesizing compounds like 2-(1-(4-bromophenyl)-2-(6-methylpyridin-2-yl)ethyl)malononitrile using a three component reaction with 2,6-lutidine, an aldehyde, and an activated methylene precursor in PEG-400 at 110°C for 12 hours. Monitoring by TLC and NMR spectroscopy showed the desired products were obtained.
IJERA (International journal of Engineering Research and Applications) is International online, ... peer reviewed journal. For more detail or submit your article, please visit www.ijera.com
This document describes a one-pot synthesis of 3,4-dihydropyrimidin-2(1H)-ones and thiones using 4-nitrophthalic acid as a catalyst under solvent-free conditions. Various aldehydes, 1,3-dicarbonyl compounds, and urea or thiourea reacted smoothly in good to excellent yields. The reaction conditions were optimized to use a 2 mol% catalyst loading at 90°C for 30 minutes. 4-Nitrophthalic acid proved to be an effective and inexpensive catalyst for this Biginelli reaction, providing advantages over other reported catalysts such as higher yields, simpler workup, and an environmentally friendly procedure. The products were characterized
A Comparison of Spectrophotometric and Oxidoreduction Potential Method for La...CrimsonpublishersMedical
Polyphenol oxidases (PPOs) oxidize phenolic compounds forming quinones, which undergo non-enzymatic reactions resulting in colored
compounds. We studied ferulic acid and catechol oxidation by Myceliophthora thermophila laccases using oxidoreduction potential (ORP or Eh) as a novel
method to determine PPO activity compared to the traditional spectrophotometric method. Eh varied time-dependently on ferulic acid and catechol
concentrations. Eh increased to a maximum value (Ehmax), then decreased irreversibly proportional with substrate concentration. The ΔEh curves of
ferulic acid and catechol oxidation at different concentrations by laccase exhibited two steps substrate oxidation: enzymatic and non-enzymatic; linear
segments with increasing and decreasing slopes (rate of ΔEh change). The Km values determined spectrophotometrically and ORP were 0.55, 0.75 and
0.39, 0.32mM for catechol and ferulic acid, respectively. The kinetic parameters (Km, Vmax) of enzymatic reaction were not significantly different between
the spectrophotometry and ORP methods. The ORP method is simple, low-cost and fast enabling the differentiation between the enzymatic and nonenzymatic phenol oxidation reactions
Similar to Quinoxaline as a potent heterocyclic moiety (20)
Congenital Agenesis Of The Corpus Callosum With Intracerebral Lipoma And Fron...iosrphr_editor
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
“Hemodynamic and recovery profile with Dexmedetomidine and Fentanyl in intrac...iosrphr_editor
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
Correlation of Estrogen and Progesterone Receptor expression in Breast Canceriosrphr_editor
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
Analytical Study of Urine Samples for Epidemiology of Urinary Tract Infection...iosrphr_editor
The current study was carried out in District Abbottabad aimed to determine the common urinary
tract infections in local community to determine the epidemiology of significant diseases in asymptomatic patients
of renal disorder. In this study a total of 1000 urine samples were examined during 3rd February to 1st April 2015
from patients attending Ayub Teaching Hospital Abbottabad by using dipstick and microscopic analysis of urine.
There were 638 females and 362 males patients examined during this period. The range of age groups is between
1.5 years to 80 years. Results of this study was reported as Pyuria 11%, Proteinuria 21.1%, Hematuria 10.4%,
Epithelial Cells 8.2%, pH 7.8 %, Granular casts 7.3%, Triple phosphate 6.6%, Calcium oxalate 6.4%, Glycosuria
6.3%, Bacteria 6.2% and mucous 4.1%. This study concludes that routing urinalysis should be performed for all
individuals to diagnose the asymptomatic diseases that will help in simple therapeutic measurements as urinalysis
is a simple step to determine the root of Urinary tract disorders.
Chest sonography images in neonatal r.d.s. And proposed gradingiosrphr_editor
BACKGROUND : Lung sonography has been used to monitor the patients of R.D.S. in
N.I.C.U. in recent times.
AIMS : To Describe and Grade the changes of R.D.S. by lung sonography.
SETTING & DESIGN : Tertiary care institutional set up in a rural medical college.
STUDY DURATION : September 2014 to May 2015. Follow-up variable, upto 2 weeks.
PROSPECTIVE, ANALYTICAL STUDY.
MATERIALS AND METHODS -This was a single institute study approved by the institutional ethics
committee. Prior informed consent was obtained from the parents. 100 consecutive patients admitted in
N.I.C.U. WITH gestational age < 36 weeks with respiratory complaints were enrolled. Chest x-ray was
obtained within few hours of admission and lung sonography was performed within 24 hours. Follow – up
sonography was performed as and when necessary. Sonography image was graded and correlated with chest
xray and clinical picture
The Comprehensive Review on Fat Soluble Vitaminsiosrphr_editor
This review article deals with brief description of fat soluble vitamins with figures and tables
showing statistical analytical data duly quoting the references wherever necessary. The word “soluble” actually
means “able to be dissolved.” Whether a vitamin is classified as 'fat-soluble' or 'water-soluble' has to do with
how the vitamin is absorbed, stored and removed from the body. Vitamins are tiny organic compounds with a
huge impact on the health and well-being of the body. The body needs a small amount of fat soluble vitamins in
order to stay in optimal health. Fat soluble vitamins play an important role in keeping the body healthy and
functioning from immune system and muscle and heart function, easy flow and clotting of blood as well as eye
health. They are critical to health and wellness–particularly reproductive health and wellness. Low-fat, no-fat
and vegan diets are woefully lacking in fat soluble vitamins. However a diet based on traditional foods can
naturally provide these vitamins. Science is still learning about many of the functions of vitamins. "Too much
vitamin A, D, or K can lead to increased levels that are unhealthy and can cause serious health consequences.
Diseased conditions leading to decreased fat absorption leads to decreased absorption of vitamins. The fatsoluble
vitamins work most safely and effectively when obtained them from natural foods within the context of a
diet rich in all their synergistic partners. If fat soluble vitamins are stored for lengthy time they generate threat
for toxicity than water soluble vitamins and such situation even aggravated, provided they are consumed in
excess. Vitamin products, above the legal limits are not considered food supplements and must be registered as
prescription or non-prescription (over-the-counter drugs) due to their potential side effects. Vitamin A and E
supplements do not provide health benefits for healthy individuals, instead they may enhance mortality, and it is
held proved that beta-carotene supplements can be harmful to smokers
Sulphasalazine Induced Toxic Epidermal Necrolysis A Case Reportiosrphr_editor
The document describes a case study of an 18-year-old female patient who developed toxic epidermal necrolysis as a severe adverse reaction to the drug sulfasalazine, which she had been taking for ankylosing spondylitis. She was admitted to the intensive care unit and treated with high dose corticosteroids, fluid replacement, and supportive care. She improved with treatment and was discharged with only post-inflammatory hypopigmentation.
Evaluation the efficacy of IVIgG in treatment of Hemolytic Disease of Newborniosrphr_editor
Hemolytic disease of newborn (HDN) is an important cause of hyperbilirubinemia in the
neonatal period,and delayed diagnosis and treatment may lead to permanent brain damage. Traditional
neonatal treatment of HDN is intensive phototherapy and exchange transfusion.Intravenous
immunoglobulin(IVIgG) has been introduced as an alternative therapy to exchange transfusion. This study was
conducted to assess the effect of IVIG in HDN .
FIBROLIPOMATOUS HAMARTOMA OF ULNAR NERVE: A RARE CASE REPORT.iosrphr_editor
Nervous fibrolipomatous hamartoma is said to be a rare tumor-like condition involving the peripheral
nerves,in which the epineurium and perineurium are enlarged and distorted by excess of fatty and fibrous tissue
s that infiltrate between and around nerve boundaries. The median nerve is more likely to develop a hamartoma
than other nerves with a predilection for the carpal tunnel.
A fibrolipomatous hamartoma – is a rare, benign, congenital lesion most commonly found in the median nerve,
usually at the level of the wrist or hand.
We report a case of this rare condition in ulnar nerve.
SELF MEDICATION PRACTICES FOR ORAL HEALTH PROBLEMS AMONG DENTAL PATIENTS IN B...iosrphr_editor
This study examined self-medication practices for oral health problems among dental patients in Bangalore, India. The study found that 100% of the 175 dental patients surveyed practiced self-medication. Toothache was the most common triggering factor reported. Analgesics and herbal remedies were commonly used for self-treatment. Most participants consulted pharmacists for advice on self-medication and would see a dentist only if problems persisted after self-medicating. The high prevalence of self-medication indicates a need for education programs to increase awareness of risks.
Clinico-haematological Profile of Falciparum Malaria in a Rural Hospital of T...iosrphr_editor
Aim: To study the clinico-haematological profile malaria in a rural hospital of Tripura.
Material and methods: A cross-sectional hospital-based study was done from at Kulai District
Hospital,Tripura. This hospital based cross sectional study was done on 60 confirmed cases of falciparum
malaria (either by peripheral smear or rapid diagnostic test) admitted in Kulai District Hospital. A case sheet
proforma was prepared and data (demographic profile,clinical feature, investigation, treatment, and
complication) from all indoor patients was collected and analyzed.
Result: Out of 60 patients, 40(66.6%) were males and 20 (33.4%) were females. Most of the patients were
between the age group 21-40 years with the highest prevalence between the age group of 21-30. Fever was the
most common symptom. Anemia was present in 42(70%) patients, out of which 6(10%) patients had severe
anemia. Thrombocytopenia was present in 36(60%) patients.Abnormal liver function tests were observed in
26(43.3%) subjects while abnormal kidney function tests were observed in16(26.6%) patients. All the 60
patients received Artemisinin based antimalarial drugs.
Conclusion: Early detection, prompt management, and adequate supportive therapy may reduce mortality due
to falciparum cerebral malaria.
Indonesian Wild Ginger (Zingiber sp) Extract: Antibacterial Activity against ...iosrphr_editor
The document summarizes a study that tested the antibacterial activity of extracts from three species of wild ginger plants from Indonesia (Zingiber zerumbet, Zingiber amaricans, and Zingiber aromaticum) against Mycoplasma gallisepticum, a pathogen that causes respiratory disease in chickens. Phytochemical analysis revealed the presence of alkaloids, flavonoids, tannins, and terpenoids in the plant extracts. Disc diffusion and minimum inhibitory concentration assays showed that ethanol extracts of dried rhizomes had the strongest inhibitory effects against the pathogen, with minimum inhibitory concentrations ranging from 7.8 to 31.2 mg/ml. The results suggest that extracts from these wild ginger plants
A case of allergy and food sensitivity: the nasunin, natural color of eggplantiosrphr_editor
Abstract: Allergies and food sensitivities can both be considered as "adverse reactions individualistic" to food.
Are pathological and individual forms because they affect a few individuals in way rather serious; immediate
or delayed reactions occur instead with simple effects histamine, or, in severe cases with respiratory and
anaphylactic shock
The eggplant (Solanum melongena L.) is known to cause food allergies in some Asian countries, but detailed
studies on allergies caused by eggplant are lacking, however, it was highlighted the presence of allergens in
edible parts of eggplant with preponderance in the peel .
The purpose of this study was to propose an extraction method rapid, efficient and cost of natural dye from
waste products from the food industry, such as the peels of eggplant, from which it was extracted, isolated and
purified the nasunin,a colored molecule in red-fuchsia.
Nasusin was tested on 58 patients to evaluate the potential sensitizing effect on the skin. The results demonstrate
that allergenic effects are negligible and therefore the nasunin can be used as a colorant in various industrial
sectors with a certain safety margin
Complete NMR Assignment of MogrosidesII A2, II E andIII A1Isolated from Luo H...iosrphr_editor
NMR analysis allowed complete assignments of three known mogrol glycosides, Mogroside IIA2 (1),
II E (2)and IIIA1 (3), isolated from the extracts of Luo Han Guo. Herein, complete 1H and 13C NMR
assignmentsof all threemogrosidesare described based on NMR experiments (1H NMR, 13C NMR, COSY,
HSQC-DEPT, HMBC, NOESY and 1DTOCSY) and mass spectral data.
Nanoemulsion and Nanoemulgel as a Topical Formulationiosrphr_editor
: Nanoemulsion is referred type of emulsion with uniform and extremely small droplet size in the range
of 20-200 nm. Nanoemulsion provides numerous advantages over other carrier such as polymeric nanoparticle
and liposomes, including low cost preparation procedure, high hydrophilic and lipophilic drug loading system
to enhance the longer shelf live upon preserving the therapeutic agents. Incorporating the preparation of
nanoemulsion with hydrogel matrix to produce nanoemulgel exhibited by the two separate systems that forming
it. Nanoemulgel possesses the properties of thixotropic, non-greasy, effortlessly spreadable, easily be removed,
emollient, not staining, soluble in water, longer shelf life, bio-friendly, translucent and agreeable appearance.
Pharmacokinetics of High-Dose Methotrexate in Egyptian Children with Acute Ly...iosrphr_editor
Aim:Since several factors have been shown to influence the clearance of methotrexate, the purpose of this study
was to identify potential relationships between patient covariates and the methotrexate clearance estimates and
deduce a pharmacokinetic model for the estimation of methotrexate clearance in Egyptian pediatric ALL
patients that may help dosage adjustment and achieve target steady-state plasma concentrations in a similar
sittings.
Patients and methods: A total of 94 pediatric patients with B-cell ALL, of whom 70 were the studied population
and 24 were the test population, were treated with four courses of HDMTX doses 2.5 gm/m2
(low-risk arm) or 5
gm/m2
(standard-/high-risk arm) given every other week by intermittent intravenous infusions over 24 hours as
a part of their treatment protocol. Patients were monitored for the 24 hour MTX concentration and the systemic
methotrexate clearance was calculated for each methotrexate dose
Epidemiology of Tuberculosis (TB) in Albania 1998-2009iosrphr_editor
Abstract : In Albania, many people erroneously think that tuberculosis (TB) is a disease of the past-an illness
that no longer constitutes a public health threat. Surveillance is an integral part of tuberculosis (TB) control.
Albania has a highTB notification rate and there are doubts about underreporting. The evolution of the
incidence of tuberculosis is presented, together with more detailed figures over the period 1998-2009. These
figures were obtained by the monthly forms (called 14/Sh) compared with the individual notification data.
Objective: To examine the distribution and sources of increased tuberculosis (TB) morbidity and reporting
system deficiencies in the Albania from 1998 through 2009. Metodology: The study is descriptive one conductet
during the period 1998-2009. The statistical analysis is based on data reported from regional level (regional
epidemiological departments) to the central level (Public Health Institute). Results: The main findings were:
discordance between the collected data (individual form) and reported data (monthly form); tuberculosis
incidence rate shows little oscillations which ranges from 6.67 to 9.2 cases/100.000 population; 50% of the
regions show a lack of information on the confirmation of diagnosis and laboratory examination type used for
confirmation. Conclusion: TB disease in high-risk populations where it is difficult to detect, diagnose, and treat;
limitations of current control measures and the need for new tests and treatments, including an effective
vaccine; improving information system, regulation of individual form and personnel training.
Total Phenol and Antioxidant from Seed and Peel of Ripe and Unripe of Indones...iosrphr_editor
Study on total phenol and antioxidantactivity ofsugar apple fruits of various solvent, part of fruits, and level of ripening. Solvent extraction used were 80% (v/v) methanol, 50% (v/v) acetone, boiling water, and 50% (v/v) ethanol. Part of fruits thatbeen used for samples were seed and peel which are normally by products of sugar apple processing, level of ripening were unripe, and ripe sugar apple fruits. Total phenol was determined by Folin-ciocalteau method. Total antioxidant was quantified by 1,1-diphenyl-2-picrylhydrazyl(DPPH) method.Therewas a difference in type of solvent, part of fruits, and level of ripeningon total phenol and antioxidant concentration of sugar apple fruits. Seeds have higher total phenol concentration than peels of this fruits. Unripe sugar apple fruits have higher total phenol and antioxidant than ripe fruit. The best solvent for phenol extraction was ethanol 50%butthe best solvent for antioxidant extraction was acetone 50%.
A Review on Step-by-Step Analytical Method Validationiosrphr_editor
When analytical method is utilized to generate results about the characteristics of drug related samples it is essential that the results are trustworthy. They may be utilized as the basis for decisions relating to administering the drug to patients. Analytical method validation required during drug development and manufacturing and these analytical methods are fit for their intended purpose. To comply with the requirements of GMP pharmaceutical industries should have an overall validation policy which documents how validation will be performed. The purpose of this validation is to show that processes involved in the development and manufacture of drug, production and analytical testing can be performed in an effective and reproducible manner. This review article provides guidance on how to perform validation characteristics for the analytical method which are utilized in pharmaceutical analysis.
A Cross Sectional Study of Ethnic Differences in Occurrence and Severity of A...iosrphr_editor
Non-steroidal anti-inflammatory drugs are the most widely used "over the counter" medication all over the world despite their complications in different major organs. Present studies envisaged for knowing the occurrence and severity of adverse drug reactions from NSAIDs in different ethnic communities of Sikkim. A cross sectional study was undertaken in the medicine outpatients department of a secondary and tertiary care hospital. The patients belonging to Nepalese, Bhutias, Lepchas ethnic communities and others community (settlers from other parts of India) were included to analyzed the data based on the age and gender, ethnicity and ADRs, drugs and ADRs. Severity assessment was done using Hartwing and Siegel scale and causality assessment by Naranjo scale. Total 109 cases of ADRs, predominating in female were detected. Nepalese were the most affected and Gastrointestinal tract (GIT) being the most affected organ in them. Diclofenac showed maximum number of ADRs in all the communities. Maximum number of cases occurred on single day use (40.36%) of drugs. All the cases were belonging to the "possible category" and the maximum being the mild (72.48%) in nature. It is advisable to consider the ethnic/racial differences equally with other factors, to improve the safety and efficacy of a drug.
Does Over-Masturbation Contribute to Chronic Prostatitis.pptxwalterHu5
In some case, your chronic prostatitis may be related to over-masturbation. Generally, natural medicine Diuretic and Anti-inflammatory Pill can help mee get a cure.
Recomendações da OMS sobre cuidados maternos e neonatais para uma experiência pós-natal positiva.
Em consonância com os ODS – Objetivos do Desenvolvimento Sustentável e a Estratégia Global para a Saúde das Mulheres, Crianças e Adolescentes, e aplicando uma abordagem baseada nos direitos humanos, os esforços de cuidados pós-natais devem expandir-se para além da cobertura e da simples sobrevivência, de modo a incluir cuidados de qualidade.
Estas diretrizes visam melhorar a qualidade dos cuidados pós-natais essenciais e de rotina prestados às mulheres e aos recém-nascidos, com o objetivo final de melhorar a saúde e o bem-estar materno e neonatal.
Uma “experiência pós-natal positiva” é um resultado importante para todas as mulheres que dão à luz e para os seus recém-nascidos, estabelecendo as bases para a melhoria da saúde e do bem-estar a curto e longo prazo. Uma experiência pós-natal positiva é definida como aquela em que as mulheres, pessoas que gestam, os recém-nascidos, os casais, os pais, os cuidadores e as famílias recebem informação consistente, garantia e apoio de profissionais de saúde motivados; e onde um sistema de saúde flexível e com recursos reconheça as necessidades das mulheres e dos bebês e respeite o seu contexto cultural.
Estas diretrizes consolidadas apresentam algumas recomendações novas e já bem fundamentadas sobre cuidados pós-natais de rotina para mulheres e neonatos que recebem cuidados no pós-parto em unidades de saúde ou na comunidade, independentemente dos recursos disponíveis.
É fornecido um conjunto abrangente de recomendações para cuidados durante o período puerperal, com ênfase nos cuidados essenciais que todas as mulheres e recém-nascidos devem receber, e com a devida atenção à qualidade dos cuidados; isto é, a entrega e a experiência do cuidado recebido. Estas diretrizes atualizam e ampliam as recomendações da OMS de 2014 sobre cuidados pós-natais da mãe e do recém-nascido e complementam as atuais diretrizes da OMS sobre a gestão de complicações pós-natais.
O estabelecimento da amamentação e o manejo das principais intercorrências é contemplada.
Recomendamos muito.
Vamos discutir essas recomendações no nosso curso de pós-graduação em Aleitamento no Instituto Ciclos.
Esta publicação só está disponível em inglês até o momento.
Prof. Marcus Renato de Carvalho
www.agostodourado.com
Basavarajeeyam is a Sreshta Sangraha grantha (Compiled book ), written by Neelkanta kotturu Basavaraja Virachita. It contains 25 Prakaranas, First 24 Chapters related to Rogas& 25th to Rasadravyas.
Osteoporosis - Definition , Evaluation and Management .pdfJim Jacob Roy
Osteoporosis is an increasing cause of morbidity among the elderly.
In this document , a brief outline of osteoporosis is given , including the risk factors of osteoporosis fractures , the indications for testing bone mineral density and the management of osteoporosis
Adhd Medication Shortage Uk - trinexpharmacy.comreignlana06
The UK is currently facing a Adhd Medication Shortage Uk, which has left many patients and their families grappling with uncertainty and frustration. ADHD, or Attention Deficit Hyperactivity Disorder, is a chronic condition that requires consistent medication to manage effectively. This shortage has highlighted the critical role these medications play in the daily lives of those affected by ADHD. Contact : +1 (747) 209 – 3649 E-mail : sales@trinexpharmacy.com
8 Surprising Reasons To Meditate 40 Minutes A Day That Can Change Your Life.pptxHolistified Wellness
We’re talking about Vedic Meditation, a form of meditation that has been around for at least 5,000 years. Back then, the people who lived in the Indus Valley, now known as India and Pakistan, practised meditation as a fundamental part of daily life. This knowledge that has given us yoga and Ayurveda, was known as Veda, hence the name Vedic. And though there are some written records, the practice has been passed down verbally from generation to generation.
Integrating Ayurveda into Parkinson’s Management: A Holistic ApproachAyurveda ForAll
Explore the benefits of combining Ayurveda with conventional Parkinson's treatments. Learn how a holistic approach can manage symptoms, enhance well-being, and balance body energies. Discover the steps to safely integrate Ayurvedic practices into your Parkinson’s care plan, including expert guidance on diet, herbal remedies, and lifestyle modifications.
Tests for analysis of different pharmaceutical.pptx
Quinoxaline as a potent heterocyclic moiety
1. IOSR Journal Of Pharmacy
(e)-ISSN: 2250-3013, (p)-ISSN: 2319-4219
www.iosrphr.org Volume 4, Issue 12 (December 2014), PP. 17-27
17
Quinoxaline as a potent heterocyclic moiety
Sujiti Srivastava,1
Janmajoy Banerjee*,1
Nomi Srestha1
Department of pharmacy, Sunsari Technical College, Dharan NEPAL
ABSTRACT: Various novel, mild, eco-friendly and efficient methods has been developed for the preparation
of quinoxaline derivatives in high yields via condensation of aromatic diamine and 1,2-dicarbonyl compounds
or alphahydroxyketones in the presence of different catalyst such as CuSO4/KMno4 , iodine, phenol similarly
by using different solvents such as water, ethanol. As part of current studies, we here in report efficient
practical techniques like- sonication (sonochemistry sythesis), heating, grinding and simple mortal-pastel
methods (mechanochemistry). However, all results suggest a mild and heterogeneous nature of these
mechanisms, shorter time of reaction and higher yield or similar to reported older methods, the review here is
to highlight some convenient methods of synthesis with keeping an eye to their various biological importances.
KEYWORDS-alphahydroxyketones, sonochemistry, antioxidantactivity.
Methods for synthesis of quinoxaline:
I. INTRODUCTION:
The current review mainly concern with the catalytic method of synthesis of quinoxaline derivatives.
Due to the important role in lead optimization as well as for the synthesis of derivatives, effective and
convenient methods are a serious need for medicinal chemistry.Quinoxaline is commonly called as or
benzopyrine. . Quinoxaline and its derivatives are mostly of synthetic origin.The fusion of one or two benzene
rings in quinoxaline and phenazine increases the number of resonance structure, which are available to these
systems. It posses the dipole moment of zero. Considering these properties, various research workers have
shown a keen interest in this small heterocyclic moiety as target structure for evaluation of many
pharmacological activities. This review includes various synthetic routes and guidelines for the development of
new quinoxalines
Nitrogen containing heterocyclic compounds are indispensable structural units for both the chemists and
biochemists.Among the various classes of benzene fused six-membered nitrogen containing heterocyclic
compounds,quinoxaline derivatives form an important class of pharmacologically active compounds.The
numbering and chemical sturucture is as shown above. Numerous quinoxaline derivatives have important
biological activity such as antibacterial[1], , anticancer[2], anti-inflammatory agents[3] antimycobial and
anticandida[4], cytotoxic[5], Antioxidant[6], Anticonvulsant[7], antiviral[8], SR protein-specific kinase-1
inhibitor[9] activity.
II. CHEMISTRY
Quinoxaline is a low melting solid, m.p 29-30˚C and is miscible with water. It is weakly basic pKa
0.56.Quinoxaline forms salts with acids. Nitration occurs only under forcing conditions (Conc. HNO3,
Oleum,90◦C) to give 5-nitroquinoxaline (1.5%) and 5, 7-dinitro- quinoxaline (24%).
2. Quinoxaline as a potent heterocyclic…
18
Oxidation of quinoxaline results in the formation of the product depending on the nature of the oxidizing agent
employed. With alkaline potassium permanganate pyrazine 2,3-dicarboxylic acid is formed, while with peracid
quinoxaline di-N-oxide results.[10]
SYNTHESIS:
1. Atghia and Beigbaghlou examined the reaction of 1,2-phenylenediamine (1 mmol) with benzil (1 mmol) in
various solvents (EtOH, THF, MeCN, EtOAc, and toluene) and also under solvent-free classical heating
conditions in the presence of different amounts of the catalyst. The best result was achieved by carrying out the
reaction in the presence of 10 mg of TiO2-Pr-SO3H in EtOH[11]
2. Sajjadifar developed a novel, mild, eco-friendly and efficient method for the preparation of quinoxaline
derivatives in high yields via a one-pot condensation of aromatic diamine and 1,2-dicarbonyl compounds in the
presence of [2-(sulfooxy)ethyl]sulfamic acid (SESA)[12].
X=CH,N
3. Karami And Khodabakhshi produced a Convenient and simple procedures for the synthesis of phenazine and
quinoxaline derivatives were developed via a reaction of o-phenylenediamines and 1,2-dicarbonyl compounds.
In addition, the synthesis of two new 1,4-benzodiazine derivatives and the catalytic activity of magnesium
sulfate heptahydrate (MgSO4·7H2O) in the room temperature condensation of o-phenylenediamines and 1,2-
dicarbonyl compounds in ethanol as solvent are reported[13].
3. Quinoxaline as a potent heterocyclic…
19
4. Heravi et al o-Iodoxybenzoic acid (IBX), a readily available hypervalent iodine (V) reagent, was found to be
highly effective in synthesis of quinoxaline derivatives, from 1,2-diketones and ophenylenediamines at room
temperature in very high yields[14]
5. Fan and Hua studied, Yb immobilized NaY zeolite catalyst (Yb/NaY) which was obtained by a hydrothermal
method and characterized by XRD, BET, FT-IR, ICP-AES, and NH3-TPD. The catalyst displayed good
catalytic activity when applied to the synthesis of quinoxalines via condensation of a-hydroxyketones with 1,2-
diamines, and could be reused several times without any loss of catalytic activity[15].
6. Nagarapu and et al synthesized Quinoxaline derivatives by a simple, efficient, one-pot, two-component
condensation of α,β-unsaturated ketones, o-phenylenediamine in the presence of a catalytic amount of 5%
WO3/ZrO2 in excellent yields.The effect of electron releasing and electron with drawing substituent on the
aromatic ring of phenacyl bromides on the reaction was investigated. Electron releasing groups and electron
withdrawing groups did not affect significantly on the yields and the reaction times. Using 1,2-diamines
possessing electron-withdrawing substituent needed longer reaction times and the yields were lower[16].
4. Quinoxaline as a potent heterocyclic…
20
7. Soleymani et al synthesized compounds based on condensation of Aryl-1,2-di amine with 1,2-di carbonyl in
the acidic condition, some new compounds was obtained from Quinoxaline family that for the first time some
new catalysts was used for increasing of efficiency and reducing of process time. Used catalysts were
CrCl2.6H2O, PbBr2 and CuSO4.5H2O compounds that preparation of these catalysts is economically, cost-
effective and saves time. All mechanisms were done in ethanol solvent at room temperature[17]
8. Sajjadifar et al described a simple, highly efficient and green procedure for the condensation of aryl and alkyl
1,2-diamines with α-diketones in the presence of catalytic amount of citric acid at room temperature . Using this
method, quinoxaline derivatives as biologically interesting compounds are produced in high to excellent yields
and short reaction times under mild and green condition. In this research, new quinoxaline derivatives were
produced.[18]
5. Quinoxaline as a potent heterocyclic…
21
9. Biswas et al developed an operationally simple and efficient cascade strategy to access substituted
isoindolo[2,1-a]quinoxalines via one step copper-catalysed C-N coupling of substituted 2H-isoindole-1-
carbaldehyde and substituted 2-halophenylamines . Another straight forward procedure to prepare substituted
isoindolo[2,1-a]quinoxalin-6(5H)-ones involving transformation of substituted 2H-isoindole-1-carboxylic acids
to acid chloride, coupling with substituted 2-iodophenylamines and copper-catalysed C-N coupling is
described[19]
10.Shi et al described an efficient and clean method for the synthesis of 1,5-benzodiazepines from o-
phenylenediamine and ketones catalyzed by sodium tetrachloroaurate(III) dihydrate under mild conditions. The
catalyst was shown to be equally effective for the synthesis of quinoxalines from o-phenylenediamine and α-
bromo ketones under the similar reaction conditions. This method produced good yields[20].
11. Yun-fei et al described Ga(ClO4)3-catalyzed reaction of 1,2-aryldiamines and α-bromoketones to afford 2-
substituted quinoxalinesbin good yields . The reaction proceeded via grinding process with 10%(molar fraction)
catalyst underbsolvent-free conditions at room temperature[21]
6. Quinoxaline as a potent heterocyclic…
22
11. Huang et al found Keggin type heteropolyacids to be an efficient and reusable catalyst for the synthesis of
biologically active quinoxaline derivatives from the condensation of 1,2-diamine with 1,2-dicarbonyl
compounds in excellent yields in water. This method provides a new and efficient protocol in terms of small
quantity of catalyst, a wide scope of substrates, and simple work-up procedure[22].
12. Cartigny et al developed a highly efficient and general iridium-difluorphos-catalyzed asymmetric
hydrogenation of diverse 2-alkyl- and 2-aryl-substituted quinoxalines into biologically and pharmaceutically
relevant 2-substituted-1,2,3,4-tetrahydroquinoxaline units has been developed. High isolated yields and
excellent enantioselectivities of up to 95% for 2-alkyl-substitutedquinoxalines and of up to 94% for 2-aryl-
substituted quinoxalines were obtained.[23]
13. Pawar et al synthesized quinoxaline derivatives in high to excellent yields in the presence of thiamine
hydrochloride (VB1) as an inexpensive, nontoxic and metal ion free catalyst at ambient temperature.[24]
14. Heravi et al found o-Iodoxybenzoic acid (IBX), a readily available hypervalent iodine (V) reagent, to be
highly effective in synthesis of quinoxaline derivatives, from 1,2-diketones and ophenylenediamines at room
temperature in very high yields.[25]
7. Quinoxaline as a potent heterocyclic…
23
15. Bandyopadhyay et al produced a microwave-induced iodine-catalyzed simple, rapid and convenient
synthesis of different types of quinoxalines via condensation of 1,2-diamines with 1,2-dicarbonyl
compounds.[26]
16.Das and Sarkar carried out an efficient environmentally benign condensation of 1,2 diketones and 1,2-
diamines for a facile synthesis of quinoxalines was carried in aqueous medium in the presence of
tetraethylammonium bromate. [27]
PHARMACOLOGICAL ACTIVITIES
9. Quinoxaline as a potent heterocyclic…
25
III. CONCLUSION
This review gives an overview of the various synthetic routes used to form a biologically rich
quinoxaline moiety.This paper proves to be helpful for further research work on the bioactive quinoxaline ring
and as an important tool for the development of better medicinal agents and newer compounds possessing
quinoxaline moiety that could be better agents in terms of efficacy and safety.
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Available online 31 May 2005