This document summarizes the career and research of a pharmaceutical chemist. It includes brief descriptions of their work synthesizing radiolabeled compounds, boranophosphate oligomers for RNAi applications at Pfizer, and a bacterial translation inhibitor at Pharmacia. Their research involved developing synthetic routes for drug targets and building blocks, optimizing reaction conditions, and exploring structure-activity relationships of compounds.
Film pore diffusion modeling for sorption of azo dye on to exfoliated graphit...Science Padayatchi
The document describes research on using exfoliated graphitic nanoplatelets (xGnPs) to adsorb the azo dye Acid Orange 7 from aqueous solutions. The effects of temperature, pH, and initial dye concentration on the adsorption process were studied. Kinetic data fit the pseudo-first-order and pseudo-second-order models well. Adsorption isotherms followed the Langmuir model. Analysis of the kinetics and isotherms provided insight into the adsorption mechanism and rate determining steps. The xGnPs were found to efficiently and effectively remove the acid dye from solutions through an exothermic adsorption process governed by chemical reaction kinetics.
This document discusses metabolic activation of natural products at the Dalian Institute of Chemical Physics, Chinese Academy of Sciences. It provides examples of their research on the metabolic activation of rutaecarpine, evodiamine, pyrrolizidine alkaloids, and strychnine. For each compound, it identifies the cytochrome P450 enzymes involved in bioactivation and describes efforts to characterize reactive metabolites through trapping and protein adduct formation. The research aims to better understand metabolism-mediated toxicity of natural products.
I am honored and humbled by receiving the Samuel Rosen award from the Surfactants and Detergents Division of the American Oil Chemist's Society at the recent annual AOCS meeting. This presentation attempts to illustrate the importance of surfactant science in delivering the performance consumers expect from the products they use everyday to make their lives cleaner, healthier and better. I intended the message to reinforce the intent and spirit of the Rosen award.
The Mannich reaction of the titanium enolate derived from D-camphor with various electrophiles stereoselectively provides the exo adduct. Reactions with Eschenmoser's salt, pyrrolidylmethylene ammonium chloride, N,N-dipyrrolidinemethane, and N-methoxy(methylene)pyrrolidine selectively form the exo adduct. In contrast, previous reactions using lithium or boron enolates of D-camphor with aminals provided mixtures of exo and endo adducts. The titanium enolate approach offers an attractive one-pot method to access exo adducts using the Mannich reaction.
This document provides information on several common methods used to measure antioxidant capacity in biological samples and foods. It describes the principles, procedures, and key measurements of assays such as ORAC, DPPH, ABTS, Folin-Ciocalteu, FRAP, CAA, HPLC, UPLC, and ELISA. These assays utilize different chemical reactions and detection methods to quantify a sample's ability to inhibit oxidation initiated by free radicals.
The document discusses research into generating and studying iminoxyl radicals. Iminoxyl radicals are intermediates generated through the oxidation of oximes, which are commonly found in drugs, pesticides, food and cosmetics. The researchers aim to cleanly generate iminoxyl radicals using O-silyl oxime ethers and study their structure and reactivity. Their experiments investigate the effects of silane substituents, solvents, sensitizers and nucleophiles on iminoxyl radical rearrangement and side product formation.
In the present study, activated carbon is prepared from Murraya koenigii Stems (MKST) and used for the adsorption of methylene blue
from aqueous solution. The nitrogen adsorption isotherms were used to characterize the pore properties of the activated carbon including
the BET surface area, pore volume and pore diameter. The specific surface area of the prepared carbon is 508 m2/g. Batch mode experiments
were conducted to study the effect of adsorbent dosage on the adsorption of methylene blue. The equilibrium data fits well with Langmuir
model with monolayer adsorption capacity of 123.46 mg/g. The adsorption kinetics was studied using pseudo-first order and pseudosecond
order models. The rate of adsorption was found to conform to pseudo-second order kinetics with a good correlation. The results
show that methylene blue interacts strongly with the prepared activated carbon and hence the adsorbent is good for the removal of
methylene blue from aqueous solution.
Film pore diffusion modeling for sorption of azo dye on to exfoliated graphit...Science Padayatchi
The document describes research on using exfoliated graphitic nanoplatelets (xGnPs) to adsorb the azo dye Acid Orange 7 from aqueous solutions. The effects of temperature, pH, and initial dye concentration on the adsorption process were studied. Kinetic data fit the pseudo-first-order and pseudo-second-order models well. Adsorption isotherms followed the Langmuir model. Analysis of the kinetics and isotherms provided insight into the adsorption mechanism and rate determining steps. The xGnPs were found to efficiently and effectively remove the acid dye from solutions through an exothermic adsorption process governed by chemical reaction kinetics.
This document discusses metabolic activation of natural products at the Dalian Institute of Chemical Physics, Chinese Academy of Sciences. It provides examples of their research on the metabolic activation of rutaecarpine, evodiamine, pyrrolizidine alkaloids, and strychnine. For each compound, it identifies the cytochrome P450 enzymes involved in bioactivation and describes efforts to characterize reactive metabolites through trapping and protein adduct formation. The research aims to better understand metabolism-mediated toxicity of natural products.
I am honored and humbled by receiving the Samuel Rosen award from the Surfactants and Detergents Division of the American Oil Chemist's Society at the recent annual AOCS meeting. This presentation attempts to illustrate the importance of surfactant science in delivering the performance consumers expect from the products they use everyday to make their lives cleaner, healthier and better. I intended the message to reinforce the intent and spirit of the Rosen award.
The Mannich reaction of the titanium enolate derived from D-camphor with various electrophiles stereoselectively provides the exo adduct. Reactions with Eschenmoser's salt, pyrrolidylmethylene ammonium chloride, N,N-dipyrrolidinemethane, and N-methoxy(methylene)pyrrolidine selectively form the exo adduct. In contrast, previous reactions using lithium or boron enolates of D-camphor with aminals provided mixtures of exo and endo adducts. The titanium enolate approach offers an attractive one-pot method to access exo adducts using the Mannich reaction.
This document provides information on several common methods used to measure antioxidant capacity in biological samples and foods. It describes the principles, procedures, and key measurements of assays such as ORAC, DPPH, ABTS, Folin-Ciocalteu, FRAP, CAA, HPLC, UPLC, and ELISA. These assays utilize different chemical reactions and detection methods to quantify a sample's ability to inhibit oxidation initiated by free radicals.
The document discusses research into generating and studying iminoxyl radicals. Iminoxyl radicals are intermediates generated through the oxidation of oximes, which are commonly found in drugs, pesticides, food and cosmetics. The researchers aim to cleanly generate iminoxyl radicals using O-silyl oxime ethers and study their structure and reactivity. Their experiments investigate the effects of silane substituents, solvents, sensitizers and nucleophiles on iminoxyl radical rearrangement and side product formation.
In the present study, activated carbon is prepared from Murraya koenigii Stems (MKST) and used for the adsorption of methylene blue
from aqueous solution. The nitrogen adsorption isotherms were used to characterize the pore properties of the activated carbon including
the BET surface area, pore volume and pore diameter. The specific surface area of the prepared carbon is 508 m2/g. Batch mode experiments
were conducted to study the effect of adsorbent dosage on the adsorption of methylene blue. The equilibrium data fits well with Langmuir
model with monolayer adsorption capacity of 123.46 mg/g. The adsorption kinetics was studied using pseudo-first order and pseudosecond
order models. The rate of adsorption was found to conform to pseudo-second order kinetics with a good correlation. The results
show that methylene blue interacts strongly with the prepared activated carbon and hence the adsorbent is good for the removal of
methylene blue from aqueous solution.
Equilibrium and kinetic studies on the adsorption of methylene blue from aque...suresh899
1) Activated carbon was prepared from Murraya koenigii stems and used to adsorb methylene blue from an aqueous solution.
2) The activated carbon had a specific surface area of 508 m2/g and was characterized as mainly microporous with some mesopores present.
3) Equilibrium studies showed that the adsorption of methylene blue onto the activated carbon fit the Langmuir isotherm model best, with a maximum adsorption capacity of 123.46 mg/g.
4) Kinetic studies found that the adsorption of methylene blue followed pseudo-second order kinetics.
Contrast Media Presentation Uploaded by SONU SHARMA
Student of B.Sc Radiography & Imaging Technology 3rd Year
at Pt.B.D.Sharma University of Health & Science ,
P.G.I.M.S. Rohtak,Haryana,India.
The document discusses the use of nanoparticles for drug delivery. It notes that nanoparticles have advantages over traditional tablets and suspensions for drug delivery due to their small size, which allows for greater bioavailability and targeting of specific tissues. The size of nanoparticles is important as it influences dissolution rate and can allow particles to cross cell membranes if small enough. The document then covers various methods for creating nanoparticles, including top-down size reduction techniques and bottom-up assembly approaches. It also discusses how particle sizing instruments like dynamic light scattering and laser diffraction can be used to characterize nanoparticles and ensure batches meet the necessary specifications for drug delivery.
1. The document discusses the covalent and electrostatic attachment of yeast cytochrome c to a fused silica surface and how its structure and function are affected.
2. Experiments examined how the protein's absorption spectra changed when covalently or electrostatically attached to the surface versus in solution under varying conditions like pH and alcohol concentration.
3. The goal was to better understand how the attachment method and external factors influence the protein's conformation and ability to perform its electron transport function.
Structural characterization of morphine by using different types of spectrosc...Shikha kamboj
Morphine is a natural opium alkaloid first isolated in 1805. It is a powerful pain reliever that acts on opioid receptors in the brain and nervous system. Spectroscopy techniques like IR, NMR, and mass spectrometry are used to characterize the molecular structure of morphine. IR spectroscopy identifies functional groups based on vibrational frequencies. NMR spectroscopy provides information on bonding and stereochemistry. Mass spectrometry identifies molecular mass and fragmentation patterns. Together these techniques allow for full structural elucidation of morphine.
Phenytoin(dilantin) is an anti-convulsant drug or anti-epileptic drug. It can be prepared from benzil, an organic compound formed by the oxidation of benzoin.
This document discusses tropane alkaloids, specifically atropine alkaloid. It summarizes that atropine alkaloid is mainly found in plants from the solanaceae family, like Atropa belladona and Datura stromonium. It then describes the isolation, biosynthesis, identification tests, chemistry and properties, structure-activity relationships, uses, and mechanism of action of atropine alkaloid.
This document summarizes a study that found benzene can be produced from the decarboxylation of benzoic acid in the presence of ascorbic acid and a transition metal catalyst. The reaction involves hydroxyl radicals generated by a Fenton-type reaction catalyzed by metals like copper and iron. Benzene production increased with ascorbic acid and hydrogen peroxide concentration up to a point, and was highest between pH 2-3. This suggests benzene could form in acidic foods and beverages containing ascorbic acid and sodium benzoate preservative.
This study synthesized four carbazole-based porous organic frameworks (Cz-POFs) with different substituents as photocatalysts for visible light reactions. The Cz-POFs were characterized using NMR, IR, UV-Vis spectroscopy, and gas adsorption analysis. Catalytic testing of the Cz-POFs and their monomer precursors in debromination, amine oxidation, and [2+2] cycloaddition reactions found that the polymer photocatalysts generally had higher activity and selectivity than the monomers. Future work will analyze the electrochemical properties and reaction mechanisms of the Cz-POFs.
This document summarizes a study that investigated the potential for photochemical reactions of two thiazide compounds, bendroflumethiazide and hydroflumethiazide, when exposed to sunlight-range illumination. Spectroscopy analysis revealed that both compounds strongly absorb UV light in specific wavelength ranges. When solutions of the compounds were illuminated over time, their absorption spectra changed, indicating photochemical reactions were occurring. However, the reaction kinetics could not be definitively determined due to interference from photoproducts also absorbing at the same wavelengths. Further separation and analysis of photoproducts using HPLC will be needed to fully characterize the photochemical reactions.
NNFCC briefing document. energy from waste the benefits of upgrading househol...NNFCC
This document summarizes the benefits of pre-treating municipal solid waste (MSW) to produce refuse derived fuel (RDF) or solid recovered fuel (SRF) before energy recovery. Pre-treating MSW through mechanical biological treatment (MBT) or mechanical heat treatment (MHT) can upgrade the waste to make it more homogeneous and suitable for gasification or pyrolysis technologies. This pre-treatment can reduce greenhouse gas emissions, improve energy conversion efficiency, lower ash content and acid gas emissions, and increase the potential for material recycling compared to direct incineration of raw MSW. However, the energy demands of MBT and MHT are higher than direct incineration. The overall environmental and economic impacts depend
This document provides an overview of Albemarle Corporation's various chemical products and services. It lists numerous chemicals they produce that are used in a wide range of industries such as oil and gas, pharmaceuticals, electronics, agriculture, and more. The chart maps out Albemarle's product portfolio and the complex web of chemical reactions and syntheses used to produce them.
Honors - Organic compounds, enzymes and digestion 1213Michael Edgar
This document discusses organic compounds and enzymes in digestion. It begins with an experiment that produces organic molecules from inorganic precursors using electricity. It then covers different types of isomers that can occur in organic compounds. Enzymes are discussed, including how their handedness, or chirality, can determine their effectiveness. Enzyme kinetics are explored, looking at factors like pH, temperature, and substrate concentration that influence reaction rates. Protein structure and function are examined, including examples of enzymes and their roles in metabolic pathways. The roles of enzymes in intracellular and extracellular digestion are compared.
A new selective synthesis of d ribonucleosides in acetonitrileAlexander Decker
This document describes a new selective synthesis of D-ribonucleosides using natural phosphate (NP) doped with potassium iodide (KI) as a catalyst. Several β-D-ribonucleosides were synthesized in good yields via a one-step reaction of silylated nucleobases with acetyl-2,3,5-tri-O-benzoyl-β-D-ribofuranose under reflux in acetonitrile. NP/KI was found to be an efficient and selective catalyst for this glycosylation, providing the desired nucleosides in up to 78% yield. The reaction mechanism is proposed to involve iodide substitution on the sugar followed by nucleophilic attack of
The document discusses various applications of nanomaterials in catalysis. It begins by introducing different types of catalysts and how nanocatalysts combine advantages of homogeneous and heterogeneous systems by having a high surface area like homogeneous catalysts while also being easily separable like heterogeneous catalysts. Several examples of nanocatalyst applications are then summarized in areas like water purification, biodiesel production, drug delivery, fuel cells, environmental protection, and solar cells. The document emphasizes how nanocatalysts provide benefits like high activity, selectivity, stability, and being energy efficient.
Naproxen is a propionic acid class nonsteroidal anti-inflammatory drug (NSAID) with the chemical formula C14H14O3. It works by blocking the production of prostaglandins. This document describes the original synthesis of naproxen in 1969 and improvements made since then to increase atom economy and reduce hazardous waste production. The proposed adapted synthesis achieves a higher atom economy of 39% by replacing halogenated reagents and coupling reactions with safer carbonylation and acetic anhydride substitution steps.
Phytoremediation of phc & salt 2011 Dr GreenbergPeter Mosley
This document discusses phytoremediation of petroleum hydrocarbons (PHC) and salt impacted soils. It provides examples of full-scale phytoremediation projects successfully meeting generic Tier 1 standards at petroleum and salt impacted sites across Canada. The key to success is transferring the science of phytoremediation from the lab to the field through the use of Plant Growth Promoting Rhizobacteria (PGPR) Enhanced Phytoremediation Systems (PEPS) which promote aggressive plant growth in impacted soils. PEPS has been used to remediate over 25 sites across Canada, with remediation levels of 30-40% per year for PHC and salinity reductions of up to
This document summarizes a review on active oxygen and its applications. It discusses the generation and physiological roles of active oxygen species in organisms, including their involvement in biochemical reactions and defense systems. It also outlines various practical applications of active oxygen species in medical treatment, material development, and environmental purification. Specific examples provided include the use of singlet oxygen in photodynamic cancer therapy, synthesis of functional materials, degradation of polymers and endocrine disruptors. Methods for generating and detecting singlet oxygen are also summarized.
The Mitsunobu reaction allows the conversion of alcohols to various functional groups using trialkyl/triaryl phosphine and dialkyl azodicarboxylate reagents. It proceeds via an oxidation-reduction mechanism. Common applications include esterification, etherification, and N-alkylation reactions. Recent advances have focused on replacing conventional reagents to improve selectivity and yields. The Mitsunobu reaction has been widely used in the synthesis of natural products and pharmaceuticals.
Equilibrium and kinetic studies on the adsorption of methylene blue from aque...suresh899
1) Activated carbon was prepared from Murraya koenigii stems and used to adsorb methylene blue from an aqueous solution.
2) The activated carbon had a specific surface area of 508 m2/g and was characterized as mainly microporous with some mesopores present.
3) Equilibrium studies showed that the adsorption of methylene blue onto the activated carbon fit the Langmuir isotherm model best, with a maximum adsorption capacity of 123.46 mg/g.
4) Kinetic studies found that the adsorption of methylene blue followed pseudo-second order kinetics.
Contrast Media Presentation Uploaded by SONU SHARMA
Student of B.Sc Radiography & Imaging Technology 3rd Year
at Pt.B.D.Sharma University of Health & Science ,
P.G.I.M.S. Rohtak,Haryana,India.
The document discusses the use of nanoparticles for drug delivery. It notes that nanoparticles have advantages over traditional tablets and suspensions for drug delivery due to their small size, which allows for greater bioavailability and targeting of specific tissues. The size of nanoparticles is important as it influences dissolution rate and can allow particles to cross cell membranes if small enough. The document then covers various methods for creating nanoparticles, including top-down size reduction techniques and bottom-up assembly approaches. It also discusses how particle sizing instruments like dynamic light scattering and laser diffraction can be used to characterize nanoparticles and ensure batches meet the necessary specifications for drug delivery.
1. The document discusses the covalent and electrostatic attachment of yeast cytochrome c to a fused silica surface and how its structure and function are affected.
2. Experiments examined how the protein's absorption spectra changed when covalently or electrostatically attached to the surface versus in solution under varying conditions like pH and alcohol concentration.
3. The goal was to better understand how the attachment method and external factors influence the protein's conformation and ability to perform its electron transport function.
Structural characterization of morphine by using different types of spectrosc...Shikha kamboj
Morphine is a natural opium alkaloid first isolated in 1805. It is a powerful pain reliever that acts on opioid receptors in the brain and nervous system. Spectroscopy techniques like IR, NMR, and mass spectrometry are used to characterize the molecular structure of morphine. IR spectroscopy identifies functional groups based on vibrational frequencies. NMR spectroscopy provides information on bonding and stereochemistry. Mass spectrometry identifies molecular mass and fragmentation patterns. Together these techniques allow for full structural elucidation of morphine.
Phenytoin(dilantin) is an anti-convulsant drug or anti-epileptic drug. It can be prepared from benzil, an organic compound formed by the oxidation of benzoin.
This document discusses tropane alkaloids, specifically atropine alkaloid. It summarizes that atropine alkaloid is mainly found in plants from the solanaceae family, like Atropa belladona and Datura stromonium. It then describes the isolation, biosynthesis, identification tests, chemistry and properties, structure-activity relationships, uses, and mechanism of action of atropine alkaloid.
This document summarizes a study that found benzene can be produced from the decarboxylation of benzoic acid in the presence of ascorbic acid and a transition metal catalyst. The reaction involves hydroxyl radicals generated by a Fenton-type reaction catalyzed by metals like copper and iron. Benzene production increased with ascorbic acid and hydrogen peroxide concentration up to a point, and was highest between pH 2-3. This suggests benzene could form in acidic foods and beverages containing ascorbic acid and sodium benzoate preservative.
This study synthesized four carbazole-based porous organic frameworks (Cz-POFs) with different substituents as photocatalysts for visible light reactions. The Cz-POFs were characterized using NMR, IR, UV-Vis spectroscopy, and gas adsorption analysis. Catalytic testing of the Cz-POFs and their monomer precursors in debromination, amine oxidation, and [2+2] cycloaddition reactions found that the polymer photocatalysts generally had higher activity and selectivity than the monomers. Future work will analyze the electrochemical properties and reaction mechanisms of the Cz-POFs.
This document summarizes a study that investigated the potential for photochemical reactions of two thiazide compounds, bendroflumethiazide and hydroflumethiazide, when exposed to sunlight-range illumination. Spectroscopy analysis revealed that both compounds strongly absorb UV light in specific wavelength ranges. When solutions of the compounds were illuminated over time, their absorption spectra changed, indicating photochemical reactions were occurring. However, the reaction kinetics could not be definitively determined due to interference from photoproducts also absorbing at the same wavelengths. Further separation and analysis of photoproducts using HPLC will be needed to fully characterize the photochemical reactions.
NNFCC briefing document. energy from waste the benefits of upgrading househol...NNFCC
This document summarizes the benefits of pre-treating municipal solid waste (MSW) to produce refuse derived fuel (RDF) or solid recovered fuel (SRF) before energy recovery. Pre-treating MSW through mechanical biological treatment (MBT) or mechanical heat treatment (MHT) can upgrade the waste to make it more homogeneous and suitable for gasification or pyrolysis technologies. This pre-treatment can reduce greenhouse gas emissions, improve energy conversion efficiency, lower ash content and acid gas emissions, and increase the potential for material recycling compared to direct incineration of raw MSW. However, the energy demands of MBT and MHT are higher than direct incineration. The overall environmental and economic impacts depend
This document provides an overview of Albemarle Corporation's various chemical products and services. It lists numerous chemicals they produce that are used in a wide range of industries such as oil and gas, pharmaceuticals, electronics, agriculture, and more. The chart maps out Albemarle's product portfolio and the complex web of chemical reactions and syntheses used to produce them.
Honors - Organic compounds, enzymes and digestion 1213Michael Edgar
This document discusses organic compounds and enzymes in digestion. It begins with an experiment that produces organic molecules from inorganic precursors using electricity. It then covers different types of isomers that can occur in organic compounds. Enzymes are discussed, including how their handedness, or chirality, can determine their effectiveness. Enzyme kinetics are explored, looking at factors like pH, temperature, and substrate concentration that influence reaction rates. Protein structure and function are examined, including examples of enzymes and their roles in metabolic pathways. The roles of enzymes in intracellular and extracellular digestion are compared.
A new selective synthesis of d ribonucleosides in acetonitrileAlexander Decker
This document describes a new selective synthesis of D-ribonucleosides using natural phosphate (NP) doped with potassium iodide (KI) as a catalyst. Several β-D-ribonucleosides were synthesized in good yields via a one-step reaction of silylated nucleobases with acetyl-2,3,5-tri-O-benzoyl-β-D-ribofuranose under reflux in acetonitrile. NP/KI was found to be an efficient and selective catalyst for this glycosylation, providing the desired nucleosides in up to 78% yield. The reaction mechanism is proposed to involve iodide substitution on the sugar followed by nucleophilic attack of
The document discusses various applications of nanomaterials in catalysis. It begins by introducing different types of catalysts and how nanocatalysts combine advantages of homogeneous and heterogeneous systems by having a high surface area like homogeneous catalysts while also being easily separable like heterogeneous catalysts. Several examples of nanocatalyst applications are then summarized in areas like water purification, biodiesel production, drug delivery, fuel cells, environmental protection, and solar cells. The document emphasizes how nanocatalysts provide benefits like high activity, selectivity, stability, and being energy efficient.
Naproxen is a propionic acid class nonsteroidal anti-inflammatory drug (NSAID) with the chemical formula C14H14O3. It works by blocking the production of prostaglandins. This document describes the original synthesis of naproxen in 1969 and improvements made since then to increase atom economy and reduce hazardous waste production. The proposed adapted synthesis achieves a higher atom economy of 39% by replacing halogenated reagents and coupling reactions with safer carbonylation and acetic anhydride substitution steps.
Phytoremediation of phc & salt 2011 Dr GreenbergPeter Mosley
This document discusses phytoremediation of petroleum hydrocarbons (PHC) and salt impacted soils. It provides examples of full-scale phytoremediation projects successfully meeting generic Tier 1 standards at petroleum and salt impacted sites across Canada. The key to success is transferring the science of phytoremediation from the lab to the field through the use of Plant Growth Promoting Rhizobacteria (PGPR) Enhanced Phytoremediation Systems (PEPS) which promote aggressive plant growth in impacted soils. PEPS has been used to remediate over 25 sites across Canada, with remediation levels of 30-40% per year for PHC and salinity reductions of up to
This document summarizes a review on active oxygen and its applications. It discusses the generation and physiological roles of active oxygen species in organisms, including their involvement in biochemical reactions and defense systems. It also outlines various practical applications of active oxygen species in medical treatment, material development, and environmental purification. Specific examples provided include the use of singlet oxygen in photodynamic cancer therapy, synthesis of functional materials, degradation of polymers and endocrine disruptors. Methods for generating and detecting singlet oxygen are also summarized.
The Mitsunobu reaction allows the conversion of alcohols to various functional groups using trialkyl/triaryl phosphine and dialkyl azodicarboxylate reagents. It proceeds via an oxidation-reduction mechanism. Common applications include esterification, etherification, and N-alkylation reactions. Recent advances have focused on replacing conventional reagents to improve selectivity and yields. The Mitsunobu reaction has been widely used in the synthesis of natural products and pharmaceuticals.
1. The document reports on a new antimicrobial hydrogel coating composed of dimethyldecylammonium chitosan and poly(ethylene glycol) diacrylate that kills bacteria and fungi.
2. The proposed antimicrobial mechanism is that the positively charged hydrogel attracts and disrupts the negatively charged microbial membranes.
3. An animal study found the hydrogel coating to be biocompatible with rabbit eye tissue and non-toxic to cells.
11.[11 18]acampaquinone a novel phenanthraquinone isolated from the whole pla...Alexander Decker
1. A novel phenanthraquinone derivative called Acampaquinone was isolated from the whole plant of Acampae praemorsa.
2. Structural elucidation using spectroscopic data revealed the structure of Acampaquinone to be 2-hydroxy-6-methoxy-1,4-phenanthraquinone.
3. This is the first report of a phenanthraquinone being isolated from Acampae praemorsa.
Tsvaygboym, J Phys Chem C 2008 v112 pp 695-700nanotech2masses
This document summarizes research on the reaction of single-walled carbon nanotubes (SWNTs) with organic peroxides. The main findings are:
1) SWNTs induce the decomposition of benzoyl peroxide, p-methoxybenzoyl peroxide, phthaloyl peroxide, and trifluoroacetyl peroxide through single electron transfer, accelerating their decomposition rates.
2) Phthaloyl peroxide showed the greatest functionalization of SWNTs of the four peroxides tested.
3) t-Butoxy radicals were found to add to SWNTs, but SWNTs did not inhibit the autoxidation of cumene by alkylper
The document summarizes an exploration of using selective aerobic oxidation reactions to convert ethylbenzene to acetophenone. A series of metal activators including Mn, Pt, Co were screened to control the reactivity of O2. The best results were obtained using Co(OAc)2 with MCBA as an activator, achieving nearly quantitative yields of acetophenone. While some success was seen with new activators, literature methods using Mn still performed the best. The goal of controlling O2 reactivity through the use of catalysts was partially achieved.
Organocatalysis uses small organic molecules rather than metals to catalyze chemical reactions. Thiourea organocatalysis specifically uses thiourea derivatives to accelerate reactions through hydrogen bonding interactions. Primary amine thiourea catalysts have many advantages including being inexpensive, non-toxic, stable, and able to catalyze reactions with high enantioselectivity. The document provides procedures for synthesizing a primary amine thiourea catalyst through Boc protection of an amino acid, formation of an amide bond with benzyl amine, Boc deprotection, and conversion to an isothiocyanate derivative.
Esters are important compounds that are used in many synthetic reactions to produce products for medicinal, cosmetic, and fuel applications. This document details a laboratory experiment where benzocaine, a local anesthetic, was synthesized from p-aminobenzoic acid using Fischer esterification. The product was analyzed and characterized using melting point, NMR, IR, and GC-MS to confirm it was benzocaine. The percent yield of 85.8% indicated a successful synthesis.
Vinyl sulfones: Click applications in bioconjugation. The resurgence of a che...Fernando Hernandez-Mateo
Applications of vinyl sulfones in the field of bioconjugations. The vinyl sulfone is a chemical function with "click-chemistry" characteristic that enable it for a rapid and efficient covalent linkage of the compounds derivatized with this function and those bearing complementay chemical functions (thiol and amines)
The Mannich reaction involves the condensation of an enolizable carbonyl compound, an aldehyde such as formaldehyde, and a primary or secondary amine. This results in an aminoalkylation and formation of a β-aminocarbonyl compound known as a Mannich base. Modifications using preformed Mannich bases and reactive substrates extend the scope and selectivity of the reaction. The Mannich reaction has wide applications in organic synthesis and for producing natural and medicinal compounds.
This document summarizes a student project on the proline-catalyzed aldol reaction of cyclohexanone with nitro-substituted benzaldehydes. The students carried out the reaction using L-proline as the organocatalyst to produce β-hydroxy carbonyl products. They analyzed the reaction mixtures by TLC and purified the products via flash chromatography. NMR spectroscopy was used to analyze the isolated products and confirm the reaction mechanism. The document provides background on aldol reactions and organocatalysis as well as details of the student project procedures, results, and acknowledgments.
nano catalysis as a prospectus of green chemistry Ankit Grover
Nanocatalysis and green chemistry prospects.
Nanocatalysts have higher activity, selectivity, and efficiency than traditional catalysts due to their high surface area to volume ratio. They can be designed for sustainability by having properties like recyclability, durability, and cost-effectiveness. Examples discussed include gold nanoparticle catalysts for oxidation reactions and magnetically separable nanoparticle catalysts. Nanocatalyst applications highlighted are water splitting for hydrogen production and storage, and fuel cells.
Isotopic Abundance Analysis of Biofield Treated Benzene, Toluene and p-Xylene...rachelsalk
Benzene, toluene and p-xylene are derivatives of benzene, generally produced from crude petroleum and have numerous applications in industry. The aim of the present study was to evaluate the impact of biofield treatment on isotopic abundance of these benzene derivatives by gas chromatography-mass spectrometry (GC-MS). Benzene, toluene and p-xylene samples were divided into two parts: control and treatment. Control part was remained as untreated and treatment part was subjected to Mr. Trivedi’s biofield treatment. Control and treated samples were characterized using GC-MS. GC-MS data revealed that isotopic abundance ratio of 13C/12C or 2H/1H (PM+1/PM) of treated samples were significantly increased from un-substituted to substituted benzene rings (where, PM- primary molecule, PM+1- isotopic molecule either for 13C/12C and/or 2H/1H). The isotopic abundance ratio of 13C/12C or 2H/1H (PM+1/PM) in benzene was decreased significantly by 42.14% as compared to control. However, the isotopic abundance ratio of (PM+1/PM) in treated toluene and p-xylene was significantly increased up to 531.61% and 134.34% respectively as compared to their respective control. Thus, overall data suggest that biofield treatment has significantly altered the isotopic abundance ratio of (PM+1/PM) in a different way for un-substituted and substituted benzenes.
Isotopic Abundance Analysis of Biofield Treated Benzene, Toluene and p-Xylene...wilhelm mendel
Benzene, toluene and p-xylene are derivatives of benzene, generally produced from crude petroleum and have numerous applications in industry. The aim of the present study was to evaluate the impact of biofield treatment on isotopic abundance of these benzene derivatives by gas chromatography-mass spectrometry (GC-MS). Benzene, toluene and p-xylene samples were divided into two parts: control and treatment. Control part was remained as untreated and treatment part was subjected to Mr. Trivedi’s biofield treatment. Control and treated samples were characterized using GC-MS. GC-MS data revealed that isotopic abundance ratio of 13C/12C or 2H/1H (PM+1/PM) of treated samples were significantly increased from un-substituted to substituted benzene rings (where, PM- primary molecule, PM+1- isotopic molecule either for 13C/12C and/or 2H/1H). The isotopic abundance ratio of 13C/12C or 2H/1H (PM+1/PM) in benzene was decreased significantly by 42.14% as compared to control. However, the isotopic abundance ratio of (PM+1/PM) in treated toluene and p-xylene was significantly increased up to 531.61% and 134.34% respectively as compared to their respective control. Thus, overall data suggest that biofield treatment has significantly altered the isotopic abundance ratio of (PM+1/PM) in a different way for un-substituted and substituted benzenes.
The document discusses nanocatalysts and their applications in chemical industry. It begins with definitions of catalyst and nanocatalyst. It then discusses different types of nanocatalysts including homogeneous nanocatalysts which are soluble in solvents and heterogeneous nanocatalysts which are insoluble. Methods for preparing both homogeneous and heterogeneous nanocatalysts are described. The document outlines several industrial applications of nanocatalysts such as in biodiesel production, water purification, drug delivery, and fuel cells. It concludes that nanocatalysts have advantages over traditional catalysts like high activity, selectivity, stability, and ease of separation.
This document summarizes research on synthesizing anionic foldamers for macromolecule delivery. It discusses how charge and secondary structure influence cell penetration, and how the research group synthesized quinoline oligomers and conjugated them to Alexa fluorophores via click chemistry. The conjugates could deliver cargo like oligonucleotides, peptides, and be used to assay for successful cell penetration. The overall goal is to develop non-toxic anionic molecules that can transport therapeutic macromolecules into cells.
6. Boranophosphate Nucleotide
Monomers
Building Blocks for RNAi Oligomer Synthesis
Pfizer, Inc – Cambridge, MA
2008-2009
7. Boranophosphates Delivered
Adenosine (N-BZ) 3.15 g
Cytidine (N-BZ) 3.56 g
Thymidine (N-BZ) 3.32 g
Guanosine (N-PAC)(O-DPC) 3.21 g
8. Optimizing Boranophosphorylation
Partial
purification
preserves
overall yield
Short reaction times
reduces side-
Working in 1 gram batches improves products
reproducibility and yield
Efficient
purification at this
step allows for use
of less pure
substrate
increasing
throughput
23. Substrate Effects in Deprotection
Heterocycles, 2003, 59, 207
OEt O
10 : 1
N HN
OBz MeOH : 1 M HCl OBz
O N O N
TBDMSO HO
O OBz O OBz
RT
TBDMSO OMe 83% OH OMe
OEt OEt
N 10 : 1 N OEt
N O MeOH : 1 M HCl HO
N O O N
Si O HO +
O O
O N O
RT 90 ºC OH H
Si O OH
24. New Protection Strategy for Uridine
1) Benzoyl group can be left on until final oligo deprotection
2) Can be removed under mild conditions prior to phosphitylation
3) Installation is a high yielding reaction
J. Am. Chem. Soc. 1992, 114, 4008-4010
J. Med. Chem., 1991, 34, 999-1002
25. Synthesis and SAR of A Bacterial
Translation Inhibitor
Pharmacia, Inc – Kalamazoo, MI
1999-2003
26. A Three Ring Pharmacophore
Ring substitution
Isosteric carboxylic
acid replacements
Linkers
HO
O
Ring substitution
H Other Sulfonamides
Br A N Linkers
B
O
O
S
O
Ring substitution N C Cl
Meta is better
Heterocycles
27. Synthetic Route
R6 R6
R6 R5 COOH R5 CO2Cl
Cl N
R5 COOH H (COCl)2
R4 R2 R4 R2
CH2Cl2 O S O CH2Cl2 O S O
R4 R2
Py N N
SO2Cl
Cl Cl
O CH2Cl2
HO O
O Py O
O
LiOH H R6 R5
H R6 R5
Br N Br NH2
Br N Dioxane R4
R4 40 oC O O
O O R2 S
R2 S O
O N Cl
N Cl
28. Direct o/p Chlorosulfonation
CO2H(Me) CO2H(Me)
G HSO3Cl G
65o-120 oC
SO2Cl
CO2H(Me) CO2H(Me)
HSO3Cl
65o-120 oC
SO2Cl
G G
29. m/o Chlorosulfonation via Diazotization
CO2Me HCl CO2Me CuCl . 2H2O CO2Me
AcOH SO2(g)
+ NaNO2 -
H2O Cl AcOH
+
G NH2 -10 oC G N
N 5 oC G SO2Cl
CO2Me HCl CO2Me CuCl . 2H2O CO2Me
G AcOH G SO2(g) G
+ NaNO2 -
H2O Cl AcOH
+
NH2 -10 oC N 5 oC SO2Cl
N
Organic Syntheses, Vol 60, p.121, (1981)
30. Convergent Synthesis of Cyanoanthranilic Acids
COOH
COOH
Cl
HO
H H
1) (COCl)2 / DMF N
SO2Cl O O
N NaCNBH3 N O S O CH2Cl2
S
H O
AcOH MeOH N C N
Cl Cl N
Et3N 2) LiOH
Dioxane O
Cl
PHA-xxx523
SAUR MIC 0.125 g/mL
2 g/mL in 5% serum
Br COOMe N C COOMe
+ CuCN
NMP Ratio = 16
Reflux
NH2 NH2
31. Synthesis of a Versatile Intermediate
OEt OH Cl
OEt further DMF
O O O
O ClSO3H N heating N (COCl)2 N
N
O O O
O 80 °C CH2Cl2
O O O
S S S
Cl Cl O Cl O
O
PHA-xxx228
External CRO
HO
O
PO H
PG
O R2 N N O
O
R2 NH2 H
R2 N N O O
1) HNR'R", base
CH2Cl2 O 2) Deprotect acid O S O
Py
N
O S R'
O R"
~ 15 gram scale Cl
32. Parallel Routes Afford Diversity
t-BuO
METHOD A O
t-BuO O
N C NH N O
NH2 1. HNR'R"
X HO
O 2. TFA O
O N C
N
O O S N C NH N O
O
O CH2Cl2, reflux Cl
S O
Cl O
X = OH N C BnO
1. HNR'R" O S
(COCl)2 O O
2. H2, Pd/C
DMF NH2 N
X = Cl N C NH R'
CH2Cl2 N O R"
BnO O
METHOD B O
O S O
Cl
33. Synthesis of A Novel
Bacterial Gyrase Inhibitor
Pharmacia, Inc – Kalamazoo, MI
2004-2005
34. Mechanism of Alkylidene Cyclization
O O
HN NH HN NH
-
O O O O
[1,5] Hydride Shift
O2N O2N
H
+
N N
O O
O
H O
HN NH N
O
- NH
O O O2N
O2N H H O
H N
+
N O
O
Verboom, W.; Reinhoudt, D. N.;
Visser, R.; Harkema, S. J. Org.
Chem. 1984, 49, 269-276.
35. Classical Morpholine Synthesis
2,6-Dimethylmorpholine is the only commercial 2,6-disubstituted morpholine.
Beilstein search reveals only 2 other 2,6-disubstituted morpholines.
Symmetrical cis morpholines are meso.
Non-symmetrical morpholines have regioselectivity problems in final step.
Intermediates Made by Classical Morpholine Synthesis-
O O
OH OH H2SO4
H
N N
R R 150 ºC N
H
Bn
Cis and trans isomers difficult to separate.
J. Het.Chem. 1977, 14, 899-904
Asymmetric synthesis is highly unlikely.
Morpholines are volatile.
36. Racemic Non-Symmetrical Analogs
H O H O H O
N N N
O O O
O2N NH O2N NH O2N NH
H H H
O O O
N N N
O O O
CF3
H O H O H O
N N N
O O O
O2N NH O2N NH O2N NH
H H H
O O O
N CF3 N N
O O O
37. Finishing the Asymmetric Synthesis
F O
O
H
O
Cl O
O N O
Unpublished N O Cl NO2
H
1) CH2Cl2, RT N Hunig's
HCl K2CO3
2) MeOH, reflux
CH3CN NO2
reflux
(2S,6S)-(-) (2S,6S)-(-)
O
H O
HN NH N
O
O2N NH
O O
H
O
N
CH3OH
reflux O
(2S,4S,4aS)-(-)-
38. Regioselectivity via Non-Symmetrical Morpholines
O
H O
HN NH N
-
O
O O O2N NH
Favored?
O2N H
H O
H N Me
O Me
+
N O
HN NH O
CF3
-
O O CF3
[1,5] hydride
O2N shift
H
+ Me
N O
O
H O
HN NH N
CF3 O
- NH
O O O2N
O2N H
H O
H N CF3
+ CF3
N O
O
Me
Me
39. A Regioselective Synthesis
O
NH2 HO Br
O
O OH N
CH3CN H TEA
+ + Br F3C
F3C RT N Cl CH2Cl2
F3C
0o C
Racemic
Commercial
F O
H
F3C O Cl O
F3C O
NaH/THF LAH/THF F3C O
O Cl NO2
N O N HCl
60o N
0o - RT
H K2CO3
CH3CN
reflux
O O
O NH NH
F3C O O O
O2N NH NH
HN NH O2N
H H
N O O O
O O N CF3
N
H O O
MeOH CF3
reflux
NO2
88 : 12
40. [1,5] Hydride Shift Mechanism
O
O O
HN NH H Ha H O H
NH H N N
O O H Ha O
O O O2N NH
O2N NH O2N
O2N Ha [1-5] shift Hb O
O NH
Hb CH3 CH3
Me N N O Hb CH3
N O irreversible N O O
CH3 CH3
O CH3
1 10a 11
Me
bond rotation
O O
HN HN
O NH O NH
O Hb
O2N O2N
O2N H HbO N O
N
Me
N Ha H CH3
Ha H CH3
O O
O CH3
9 Me 10b CH3
12
PNU-286607