This document describes an optimized process for synthesizing 7-ethyltryptophol, a key starting material for the non-steroidal anti-inflammatory drug etodolac. The process involves reacting 2-ethylphenyl hydrazine hydrochloride with 2,3-dihydrofuran in the presence of concentrated sulfuric acid as a catalyst in a water/dimethylacetamide solvent system. This method yields 7-ethyltryptophol in 75% yield with high purity in an easy, inexpensive, and operationally simple process without the need for purification. Testing different acid catalysts and solvent systems showed concentrated sulfuric acid and a water/dimethylacetamide mixture provided the best conversion and yield.
This slide discusses about basic indole nucleus, its chemistry, synthesis, reactions and medicinal uses of Indolyl derivatives..Indole is basically fused heterocyclic compound
This slide discusses about basic indole nucleus, its chemistry, synthesis, reactions and medicinal uses of Indolyl derivatives..Indole is basically fused heterocyclic compound
Schmidt rearrangement, B.PHARM 4 SEM, pharmceutical organic chemSAKSHI BHATT
SCHMIDT REARRANGEMENT, A NAMING REACTION.
Mechanism of production of amines, imines, amides & nitrile from Aldehyde, ketone, tertiary alcohols, alkenes & carboxylic acid
Introduction, classification, isolation, purification, biological activity of alkaloids, general methods of structural determination of alkaloids, structural elucidation of Morphine, Reserpine and Emetine
Synthesis, Reactions resonance, Reactivity and uses of naphthalene, Anthracene, Phenanthrene, naphthol, Anthraquinone and phenanthroquinone, diphenyl methane and triphenyl methane
B. Pharm. (Honours) Part-IV Practical, Medicinal Chemistry-II, MANIKImran Nur Manik
2. Medicinal Chemistry-II: (Marks-30)
Synthesis of at least two important members of the following groups of drugs: sulphonamides, antimalarials, antibiotics, barbiturates. adrenergic agents, antihistamines and antineoplastic agents.
Comparative Study and Analysis of Image Inpainting TechniquesIOSR Journals
Abstract: Image inpainting is a technique to fill missing region or reconstruct damage area from an image.It
removes an undesirable object from an image in visually plausible way.For filling the part of image, it use
information from the neighboring area. In this dissertation work, we present a Examplar based method for
filling in the missing information in an image, which takes structure synthesis and texture sysnthesis together.
In exemplar based approach it used local information from an image to patch propagation.We have also
implement Nonlocal Mean approach for exemplar based image inpainting.In Nonlocal mean approach it find
multiple samples of best exemplar patches for patch propagation and weight their contribution according to
their similarity to the neighborhood under evaluation. We have further extended this algorithm by considering
collaborative filtering method to synthesize and propagate with multiple samples of best exemplar patches. We
have to preformed experiment on many images and found that our algorithm successfully inpaint the target
region.We have tested the accuracy of our algorithm by finding parameter like PSNR and compared PSNR
value for all three different approaches.
Keywords: Texture Synthesis, Structure Synthesis, Patch Propagation ,imageinpainting ,nonlocal approach,
collabrative filtering.
Schmidt rearrangement, B.PHARM 4 SEM, pharmceutical organic chemSAKSHI BHATT
SCHMIDT REARRANGEMENT, A NAMING REACTION.
Mechanism of production of amines, imines, amides & nitrile from Aldehyde, ketone, tertiary alcohols, alkenes & carboxylic acid
Introduction, classification, isolation, purification, biological activity of alkaloids, general methods of structural determination of alkaloids, structural elucidation of Morphine, Reserpine and Emetine
Synthesis, Reactions resonance, Reactivity and uses of naphthalene, Anthracene, Phenanthrene, naphthol, Anthraquinone and phenanthroquinone, diphenyl methane and triphenyl methane
B. Pharm. (Honours) Part-IV Practical, Medicinal Chemistry-II, MANIKImran Nur Manik
2. Medicinal Chemistry-II: (Marks-30)
Synthesis of at least two important members of the following groups of drugs: sulphonamides, antimalarials, antibiotics, barbiturates. adrenergic agents, antihistamines and antineoplastic agents.
Comparative Study and Analysis of Image Inpainting TechniquesIOSR Journals
Abstract: Image inpainting is a technique to fill missing region or reconstruct damage area from an image.It
removes an undesirable object from an image in visually plausible way.For filling the part of image, it use
information from the neighboring area. In this dissertation work, we present a Examplar based method for
filling in the missing information in an image, which takes structure synthesis and texture sysnthesis together.
In exemplar based approach it used local information from an image to patch propagation.We have also
implement Nonlocal Mean approach for exemplar based image inpainting.In Nonlocal mean approach it find
multiple samples of best exemplar patches for patch propagation and weight their contribution according to
their similarity to the neighborhood under evaluation. We have further extended this algorithm by considering
collaborative filtering method to synthesize and propagate with multiple samples of best exemplar patches. We
have to preformed experiment on many images and found that our algorithm successfully inpaint the target
region.We have tested the accuracy of our algorithm by finding parameter like PSNR and compared PSNR
value for all three different approaches.
Keywords: Texture Synthesis, Structure Synthesis, Patch Propagation ,imageinpainting ,nonlocal approach,
collabrative filtering.
Effective Waste Management and Environmental ControlIOSR Journals
There is wide spread interest in the world today in the methods that enable the re-use of waste.
According to Webster’s Mew Practical Dictionary, ‘Waste’ means “Thrown away as worthless after being used.
i.e. of no further use to a person, animal or plant; contrary to this opinion, it has been discovered that what is
regarded as waste or worthless, when worked upon can be manipulated to generated or produce materials that
are beneficial for the use of man.
This paper throw light into how waste resources can be control by analysis the theories of waste
management, recycling, re-use disposal and compositing from organic wastes and ways by which farm and
municipal waste can be worked upon to produce materials that are beneficial for the use of man
Industrial Process Management Using LabVIEWIOSR Journals
Nowadays process management is a tedious task in the industry. We plan to propose a LabVIEW
based intelligent multi parameter monitoring system designed using RS232 and Microcontroller aids in the
measurement and control of various Global Parameters. For data collection in the industry is a difficult task in
real time execution of events with industrial process control and automation. We proposed two slaves for
measuring various industrial parameters to monitor and control industrial process. Data acquired from each
slave is processed and sent to Master that compile data received from different slaves and send this information
to the system configured with LabVIEW platform. This enables us to view and track the online changes
encountered in the particular parameter of all the parameters. One of the main advantages of this proposal is, it
allows us to view all the parameter readings simultaneously on the front panel in LabVIEW. The Graph drawn
on the front panel keeps on tracking the changes on the parameter. The parameters supported by this project
includes: current, voltage, temperature, frequency, light intensity, logic switches, water level identifier, and
alarm. This Project can be implemented in any of the process industries where there is a need for Simultaneous
and fast acquiring of data and control
Analysis characteristics of power PV cells and wind turbine from power genera...IOSR Journals
This paper presents the implementation of a generalized photovoltaic model using Matlab Simulink
software package, which can be representative of PV cell, module, and array for easy use on simulation
platform. The proposed model is designed with a user-friendly icon and a dialog box like Simulink block
libraries. This makes the generalized PV model easily simulated and analyzed in conjunction with power
electronics for a maximum power point tracker. Taking the effect of sunlight irradiance and cell temperature
into consideration, the output current and power characteristics of PV model are simulated and optimized using
the proposed model. This enables the dynamics of PV power system to be easily simulated, analyzed, and
optimized.
For Wind Turbine modeling and simulation of wind driven electricity generation system or WECS (an
acronym for Wind Energy Conversion System) has been done. Our aim is to design and test a power 300W
capacity, operating at 3 m/s to 6 m/s , induction permanent magnet generator Matlab simulation. The different
components of a wind energy system namely the wind turbine, generator, rectifier, as per the scope of this
project following which the design steps and modeling of the system in Matlab simulation environment -
Simulink was undertaken
Novel Way to Isolate Adipose Derive Mesenchymal Stem Cells & Its Future Clini...IOSR Journals
Abstract: Adipose-derived stem cells (ADSCs), were isolated from discarded human fat tissue, obtained from csection with our recently modified methods, in Stem Cell & Regenerative Medicine Lab, VSBT. Here we develop
two methods to isolate Adipose derived mesenchymal stem cells with enzyme digestion and use of
phosphatidylcholine and deoxycholate. Surface protein expression was analyzed by flow cytometry to
characterize the cell phenotype. The multi-lineage potential of ADSCs was testified by differentiating cells with
adipogenic inducer. ADSCs can be cultured in vitro for up to one month without passage. Also, the flow
cytometry analysis showed that ADSCs expressed high levels of stem cell related surface marker CD105.
ADSCs have strong proliferation ability, maintain their phenotypes, and have stronger multi-differentiation
potential. The molecular basis of ADSC differentiation was studied using bioinformatics tools with an aim to
identify the key proteins involved in differentiation, such that they could be used as potential targets for drug
development for the treatment of obesity. The key proteins involved were found to be PPARG and C/EBPα. The
structures of the proteins were retrieved from MMDB (Molecular Modelling Database) and PDB (Protein Data
Bank) respectively. Key Words: Adipose-derived stem cells, Mesenchymal stem cells, Enzyme digestion, Phosphatidylcholine, Deoxycholate, PPARG, C/EBPα, etc.
Performance and Evaluation of Data Mining Techniques in Cancer DiagnosisIOSR Journals
Abstract: We analyze the breast Cancer data available from the WBC, WDBC from UCI machine learning with
the aim of developing accurate prediction models for breast cancer using data mining techniques. Data mining
has, for good reason, recently attracted a lot of attention, it is a new Technology, tackling new problem, with
great potential for valuable commercial and scientific discoveries. The experiments are conducted in WEKA.
Several data mining classification techniques were used on the proposed data. There are many classification
techniques in data mining such as Decision Tree, Rules NNge, Tree random forest, Random Tree, lazy IBK. The
aim of this paper is to investigate the performance of different classification techniques. The data breast cancer
data with a total 286 rows and 10 columns will be used to test and justify the different between the classification
methods and algorithm.
Keywords - Machine learning, data mining Weka, classification, breast cancer
Reduction of Side Lobes by Using Complementary Codes for Radar ApplicationIOSR Journals
The analysis of new types of Complementary direct sequence complex signals which have synthesized
with well – know code sequences like Barker, Walsh, Golay, and complementary codes. Build on the
autocorrelation function (ACF) and ambiguity function (AF) of signals, the numerical method estimates the
volume of side lobes separately for each signal. The results obtained show that the signals, which have a low
volume of side lobes, means of approximately zero in by using complementary codes with compare to different
codes
Binary Discourse in U.S. Presidential Speeches from FDR to Bush IIIOSR Journals
The contemporary study of American Presidential rhetoric is of great significance. Politics is very largely the use of language. Presidential speech and action increasingly reflect the opinion that speaking is governing. In fact, the power of the presidency depends on its ability to persuade. The application of power is often legitimized through rhetorical persuasion; and, in the case of American Presidents, such power, and its associated rhetoric, becomes the fulcrum upon which many global issues turn
Stellar Measurements with the New Intensity FormulaIOSR Journals
In this paper a linear relationship in stellar optical spectra has been found by using a
spectroscopical method used on optical light sources where it is possible to organize atomic and ionic data.
This method is based on a new intensity formula in optical emission spectroscopy (OES). Like the HR-diagram ,
it seems to be possible to organize the luminosity of stars from different spectral classes. From that organization
it is possible to determine the temperature , density and mass of stars by using the new intensity formula. These
temperature, density and mass values agree well with literature values. It is also possible to determine the mean
electron temperature of the optical layers (photospheres) of the stars as it is for atoms in the for laboratory
plasmas. The mean value of the ionization energies of the different elements of the stars has shown to be very
significant for each star. This paper also shows that the hydrogen Balmer absorption lines in the stars follow
the new intensity formula.
Wireless Network Security Architecture with Blowfish Encryption ModelIOSR Journals
Abstract: In this research paper ,we developed a model for a large network, wireless nodes are interconnected and each can be considered as a node processor that offer services to other node processors connected to a specific network. A very high proportion of the nodes that offer services need to carry out an authentication process so as to make an access request to the node offering the service. In this context, an integrated reconfigurable network security architecture moved to the application layer has become the need of the day for secure wireless data sharing. The security schemes of the seven layer OSI architecture need to be placed intrinsically in the wireless node itself and should be capable of supporting the MAC layer, IP address based layer and the routing protocols of the network layer. This work focuses on the use of emulator and embedded hardware architectures for wireless network security. In this work, the individual nodes can have a unique security signature pattern maintained by respective wireless nodes using an encryption algorithm and this is made dynamic. The metrics includes latency, throughput, Scalability, Effects of data transfer operation on node processor and application data located in the processor Keywords:Wireless Network security, Embedded hardware, Reconfigurable architecture, blowfish algorithm
Congestion Control in Manets Using Hybrid Routing ProtocolIOSR Journals
Abstract : As the network size increases the probability of congestion occurrence at nodes increases. This is because of the event driven nature of ad hoc networks that leads to unpredictable network load. As a result congestion may occur at the nodes which receive more data than that can be forwarded and cause packet losses. In this paper we propose a hybrid scheme that attempts to avoid packet loss due to congestion as well as reduce end to end delay in delivering data packets by combining two protocols- Destination sequenced distance vector routing (DSDV), which is a table driven or proactive protocol and Improved Ad-hoc on demand vector routing (IAODV) which is an on-demand or reactive protocol that reduces packet loss due to congestion. The strategy adopted is use DSDV for path selection and if congestion occurs than switch over to IAODV. The routing performance of this model is then compared with IAODV and DSDV in terms of end to end delay, throughput and packet delivery fraction. Keywords- DSDV, Hybrid protocol, AODV, IAODV, MANET
Leather Quality Estimation Using an Automated Machine Vision SystemIOSR Journals
In the presented work, it is proposed to design the feature vector of the parameters of leather
material in order to completely define the quality of the leather material. The proposed parameters are holes,
cracks, spots, cuts, and roughness etc.. The defects are localized according to their position on leather surface,
their size and shape. The histogram analysis method is proposed to be developed for use with very low-level
image features, such as color and luminance and is used as an image descriptor for color-matching
requirements. In the present scenario, it is observed that the leather quality is highly sensitive to surface finish
of the leather material. Manually it is not possible always to inspect each area of the leather surface under test
because of heavy lot of material and it is time consuming too. The main problem during the inspection is that
how to achieve the repeatable quality at regular interval. Therefore, in order to get the authentic leather
quality, it is required to have a set of features that could be given some numerical value so that the quality can
be justified in quantified manner. A machine vision system offers a fair solution in order to solve this problem.
In the proposed work, we propose to deduce some mathematical parameters besides size and location that are arranged in a vector so as to determine the leather quality
Synthesis, Characterization, and Antibacterial Activity of Some Novel 5-Chlor...IJERA Editor
The development of potential antibacterial requires the synthesis of a new series of 5- Chloroisatin derivatives incorporating various aromatic aldehydes in the case 1,3-Dipolar Cycloaddition including Nitrile oxide, as well as the cycloaddition Alcyne-Azide Catalytic with Copper. The charcterization of the structure of the synthesized compounds was confirmed by means of their IR, 1H-NMR and 13C-NMR spectral data. In addition, the antibacterial properties in vitro were tested against certain microorganisms using the disk diffusion technique. A majority of compounds show better activity against several of the microorganisms.
An efficient synthesis, characterization and antibacterial activity of novel ...iosrjce
IOSR Journal of Applied Chemistry (IOSR-JAC) is a double blind peer reviewed International Journal that provides rapid publication (within a month) of articles in all areas of applied chemistry and its applications. The journal welcomes publications of high quality papers on theoretical developments and practical applications in Chemical Science. Original research papers, state-of-the-art reviews, and high quality technical notes are invited for publications.
Design, Synthesis, Biological Evaluation, and In Silico ADMET Studies of 1,8-...BRNSS Publication Hub
In the present study, 1,8-naphthyridine-3-carboxylic acid derivatives (5a1, 5a2, 5b1, and 5b2) were
designed, synthesized, and screened for their in vitro H1-antihistaminic activity. H1R inhibitory activity
of the synthesized derivatives was calculated by the modified Van Arman technique, histamine-induced
bronchoconstriction in guinea pigs. A good bronchorelaxant effect of compounds was observed in
histamine-contracted guinea pig tracheal chain through H1-receptor antagonism. In addition, the
hypothetically resulted compounds are checked for their reliability on other in silico drug designing
online web services like SwissADME predictor. In silico ADMET analysis results show that all the
derivatives had negligible toxicity, good absorption, and solubility profile. These compounds may serve
as possible lead for establishing safe and effective antihistaminic agent(s).
Design, synthesis, characterization and biological evaluation of 3- (4-(7-chl...iosrjce
Novel thiazolidinone derivatives TQ-VI(1-10) were designed, synthesized and screened for
antimicrobial activity. Synthesis of 3-(4-(7-chloro-2-(4-chlorophenyl) 4-oxo-quinazolin-3(4H)-yl) phenyl) -
2-arylthiazolidin-4-one TQ-VI(1-10) have been achieved from the starting material 2-amino-4-chlorobenzoic
acid TQ-I on cyclization with p-chlorobenzoyl chloride TQ-II to yield 7-chloro-2-(4-chlorophenyl)-4H-3,1-
benzoxazin-4-one,TQ-III, which on treatment with p-phenylindiamine gave 3-(4-aminophenyl)-7-chloro-2-(4-
chlorophenyl)quinazolin-4(3H)-one, TQ-IV in good yield. Then, TQ-IV on reaction with substituted aromatic
aldehydes converted to TQ-V(1-10), which on cyclization with thioglycolic acid gave TQ-VI (1-10). All the
synthesized compounds have been characterized on the basis of IR,
1
H-NMR and mass spectral data. The
compounds containing 4-OH, 4-OCH3 and 3,4,5-(OCH3)3 showed good activity. The title compounds were
screened for qualitative (zone of inhibition) and quantitative antimicrobial activity (MIC) by agar cup plate
method and serial dilution technique, respectively. Among the synthesized compounds in the series, the
compound TQVI4 and TQVI5 were found to exhibit significant antifungal activity at lower concentration of
31.25 µg/ml, against A.niger. The compound TQVI5 and TQVI4 showed zone of inhibition of 17mm and 15mm
against A.niger and C.albicans respectively which is comparable to that of standard drug. The rest of the
analogues in the series displayed weak to moderate antimicrobial activity when compared to the standard
positive controls Ampicillin and Amphotericin B.
Facial and Simple Synthesis of Some New (Pyrazole and Triazole) Coumarin Deri...IOSRJAC
2-oxo-2H-coumarin-3-carbohydrazide (2) which prepared from the reaction of ethyl-2-oxo-2Hcoumarin-3-carboxylate (1) with hydrazine hydrate in ethanol containing a catalytic amount of piperidine mixture consider a good and available starting intermediate for synthesis of series of functionalized coumarins. So, compound (2) was utilized as a key for the synthesis of some new (pyrazole, triazole)-2H- coumarin-2-one derivatives by the reaction with some selected reagents.
Research Inventy : International Journal of Engineering and Scienceresearchinventy
Research Inventy : International Journal of Engineering and Science is published by the group of young academic and industrial researchers with 12 Issues per year. It is an online as well as print version open access journal that provides rapid publication (monthly) of articles in all areas of the subject such as: civil, mechanical, chemical, electronic and computer engineering as well as production and information technology. The Journal welcomes the submission of manuscripts that meet the general criteria of significance and scientific excellence. Papers will be published by rapid process within 20 days after acceptance and peer review process takes only 7 days. All articles published in Research Inventy will be peer-reviewed.
Synthesis, spectral characterization and bioactivity studies of some S-substi...Jing Zang
A new series of 5-(4-Chlorophenyl)-1,3,4-Oxadiazol-2-thiol derivatives was prepared from 4-chlorobenzoic acid (1) by converting it successively into corresponding ester (2), carbohydrazide (3) and 5-(4-Chlorophenyl)-1,3,4-Oxadiazol-2-thiol (4). Finally the target compounds, 6a-l, were synthesized by stirring 4 with different electrophiles, 5a-l, in DMF using NaH as weak base and activator. The proposed structures of newly synthesized compounds were confirmed by spectroscopic techniques such as 1H-NMR, 13C-NMR, HR-MS and EI-MS. All synthesized compounds were evaluated for their anti-bacterial, antifungal, cytotoxicity and enzyme inhibition activities. The compounds, 6e and 6g exhibited significant inhibition activity against acetyl cholinesterase enzyme (AChE) and 6j moderate activity against butyryl cholinesterase enzyme (BChE). The molecule, 4 exhibited good MIC (minimum inhibitory concentration) value against all the bacterial and fungal strains taken into account.
Synthesis And Antibacterial Activity Of 3-[(3-Phenyl-5-Thioxo-1, 5-Dihydro-4h...inventionjournals
A series of 3-[(3-phenyl-5-thioxo-1,5-dihydro-4H-1,2,4-triazol-4-yl)imino]-1,3-dihydro-2Hindole-2-one derivatives were synthesised through the nucleophilic substitution at carbonyl carbon of Isatin. Structure of synthesized compounds were elucidated by using IR, 1H NMR & 13C NMR spectrometry. Synthesised compounds showed significant antibacterial activity against E.coli (ATCC 35218), S.aureus (ATCC 25323), E.faecalis (Clinical isolate), K. Pneumonia, P. aeruginosa (ATCC 27893) using agar well diffusion method.
Syntheses and Characterizations of Some New N-alkyl, Isoxazole and Dioxazole ...IJAEMSJORNAL
N-alkyl and cycloadducts derivatives of 5-Chloroisatin were synthesized in good to excellent yields. The method evidences a selective N-alkylation when using 1,2-bis (2-chloroethoxy) ethane as efficient spacer at room temperature on the 5-Chloroisatin moiety. A general method for the 1,3-dipolar cycloaddition of 4-Chlorobenzaldoxime to alkynes provides a useful alternative route to get newisoxazole et dioxazole derivatives.
Synthesis and Characterization O-, M- and Para-Toluyl Thiourea Substituted Pa...IOSR Journals
Abstract: Six new derivatives of carbonyl thiourea comprises of o-,m- and p-toluyl at one end of Nitrogen atom and p-methylpyridine or ethyl pyridine at another one end of Nitrogen atom has been synthesized. The compounds are, 2-methyl-N-[(4-methylpyridine-2-yl) carbamothiol] benzamide (I), 3-methyl-N-[(4-methylpyridine-2-yl) carbamothiol] benzamide (II) and 4-N-[(4-methylpyridine-2-yl) carbamothiol] benzamide (III) for Toluyl-MP while 2-methyl-N-[(2-pyridine-2-yl-ethyl) carbamothiol] benzamide (IV), 3- methyl-N-[(2-pyridine-2-yl-ethyl) carbamothiol] benzamide (V) and 4- methyl-N-[(2-pyridine-2-yl-ethyl) carbamothiol] benzamide (VI) for isomer Toluidal-AEP have been successfully synthesized and characterized by elemental analysis, Infrared Spectroscopy analysis (FT-IR), Nuclear Magnetic Resonance Spectroscopy (NMR) and Ultraviolet-visible (UV-vis). All products shown stretching modes of ν(N-H), ν(C=O), ν(C-N), and ν(C=S) around 3276 cm-1, 1671 cm-1, 1315cm-1 and 1148 cm-1 respectively. All products shown two maximum absorption around 262 nm and 290 nm respectively for carbonyl C=O and thione C=S chromophore. Those both values contributed by n -п* transition. 1H nuclear magnetic resonance spectrum showed presence of aromatic, methyl, methine and amide protons except for product III. All products showed presence of carbon thione in 13C nuclear magnetic resonance except for product III. Ionophor interpretation with acetate anion shows color changes by naked eye for compound (I) and (III).
Synthesis, Molecular Docking and Antimicrobial Evaluation of New Tetrahydrobe...ijtsrd
A series of novel derivatives of Tetrahydrobenzothienopyrimidine hydrazone were synthesized and product structure was elucidated by 1NMR, C13NMR and mass spectroscopy. The synthesized compounds were evaluated against fungal and bacterial strains. The synthesized compounds showed significant antibacterial activity against Staphylococcus aureus MTCC 96, Staphylococcus pyrogenes MTCC 442, and Escherichia coli MTCC 443, Pseudomonas aeruginosa MTCC 1688 and against fungal strains Candida albicans MTCC 227, Aspergillus niger MTCC 282, Aspergillus clavatus MTCC 1323. Some derivatives showed promising result against gram positive, gram negative bacterial and fungal strains than standard drug ampicillin and grieseofulvin. In- silico molecular docking studies of the synthesized compounds was done by using GRIP batch docking method of Vlife MDS 3.0 software to study their observed activity which showed a significant correlation between the binding score and biological activity for synthesized compounds. Neetu Chopra | Kiranpreet kaur | Sanjeev Kumar "Synthesis, Molecular Docking and Antimicrobial Evaluation of New Tetrahydrobenzothienopyrimidine Derivatives" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-2 | Issue-6 , October 2018, URL: http://www.ijtsrd.com/papers/ijtsrd18756.pdf
Similar to A optimized process for the synthesis of a key starting material for etodolac, a non steroidal anti- inflammatory drug. (20)
Multi-source connectivity as the driver of solar wind variability in the heli...Sérgio Sacani
The ambient solar wind that flls the heliosphere originates from multiple
sources in the solar corona and is highly structured. It is often described
as high-speed, relatively homogeneous, plasma streams from coronal
holes and slow-speed, highly variable, streams whose source regions are
under debate. A key goal of ESA/NASA’s Solar Orbiter mission is to identify
solar wind sources and understand what drives the complexity seen in the
heliosphere. By combining magnetic feld modelling and spectroscopic
techniques with high-resolution observations and measurements, we show
that the solar wind variability detected in situ by Solar Orbiter in March
2022 is driven by spatio-temporal changes in the magnetic connectivity to
multiple sources in the solar atmosphere. The magnetic feld footpoints
connected to the spacecraft moved from the boundaries of a coronal hole
to one active region (12961) and then across to another region (12957). This
is refected in the in situ measurements, which show the transition from fast
to highly Alfvénic then to slow solar wind that is disrupted by the arrival of
a coronal mass ejection. Our results describe solar wind variability at 0.5 au
but are applicable to near-Earth observatories.
This pdf is about the Schizophrenia.
For more details visit on YouTube; @SELF-EXPLANATORY;
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Richard's entangled aventures in wonderlandRichard Gill
Since the loophole-free Bell experiments of 2020 and the Nobel prizes in physics of 2022, critics of Bell's work have retreated to the fortress of super-determinism. Now, super-determinism is a derogatory word - it just means "determinism". Palmer, Hance and Hossenfelder argue that quantum mechanics and determinism are not incompatible, using a sophisticated mathematical construction based on a subtle thinning of allowed states and measurements in quantum mechanics, such that what is left appears to make Bell's argument fail, without altering the empirical predictions of quantum mechanics. I think however that it is a smoke screen, and the slogan "lost in math" comes to my mind. I will discuss some other recent disproofs of Bell's theorem using the language of causality based on causal graphs. Causal thinking is also central to law and justice. I will mention surprising connections to my work on serial killer nurse cases, in particular the Dutch case of Lucia de Berk and the current UK case of Lucy Letby.
Richard's aventures in two entangled wonderlandsRichard Gill
Since the loophole-free Bell experiments of 2020 and the Nobel prizes in physics of 2022, critics of Bell's work have retreated to the fortress of super-determinism. Now, super-determinism is a derogatory word - it just means "determinism". Palmer, Hance and Hossenfelder argue that quantum mechanics and determinism are not incompatible, using a sophisticated mathematical construction based on a subtle thinning of allowed states and measurements in quantum mechanics, such that what is left appears to make Bell's argument fail, without altering the empirical predictions of quantum mechanics. I think however that it is a smoke screen, and the slogan "lost in math" comes to my mind. I will discuss some other recent disproofs of Bell's theorem using the language of causality based on causal graphs. Causal thinking is also central to law and justice. I will mention surprising connections to my work on serial killer nurse cases, in particular the Dutch case of Lucia de Berk and the current UK case of Lucy Letby.
A brief information about the SCOP protein database used in bioinformatics.
The Structural Classification of Proteins (SCOP) database is a comprehensive and authoritative resource for the structural and evolutionary relationships of proteins. It provides a detailed and curated classification of protein structures, grouping them into families, superfamilies, and folds based on their structural and sequence similarities.
Observation of Io’s Resurfacing via Plume Deposition Using Ground-based Adapt...Sérgio Sacani
Since volcanic activity was first discovered on Io from Voyager images in 1979, changes
on Io’s surface have been monitored from both spacecraft and ground-based telescopes.
Here, we present the highest spatial resolution images of Io ever obtained from a groundbased telescope. These images, acquired by the SHARK-VIS instrument on the Large
Binocular Telescope, show evidence of a major resurfacing event on Io’s trailing hemisphere. When compared to the most recent spacecraft images, the SHARK-VIS images
show that a plume deposit from a powerful eruption at Pillan Patera has covered part
of the long-lived Pele plume deposit. Although this type of resurfacing event may be common on Io, few have been detected due to the rarity of spacecraft visits and the previously low spatial resolution available from Earth-based telescopes. The SHARK-VIS instrument ushers in a new era of high resolution imaging of Io’s surface using adaptive
optics at visible wavelengths.
THE IMPORTANCE OF MARTIAN ATMOSPHERE SAMPLE RETURN.Sérgio Sacani
The return of a sample of near-surface atmosphere from Mars would facilitate answers to several first-order science questions surrounding the formation and evolution of the planet. One of the important aspects of terrestrial planet formation in general is the role that primary atmospheres played in influencing the chemistry and structure of the planets and their antecedents. Studies of the martian atmosphere can be used to investigate the role of a primary atmosphere in its history. Atmosphere samples would also inform our understanding of the near-surface chemistry of the planet, and ultimately the prospects for life. High-precision isotopic analyses of constituent gases are needed to address these questions, requiring that the analyses are made on returned samples rather than in situ.
A optimized process for the synthesis of a key starting material for etodolac, a non steroidal anti- inflammatory drug.
1. IOSR Journal of Applied Chemistry (IOSR-JAC)
e-ISSN: 2278-5736.Volume 4, Issue 5 (May. – Jun. 2013), PP 03-05
www.iosrjournals.org
www.iosrjournals.org 3 | Page
A optimized process for the synthesis of a key starting material
for etodolac, a non steroidal anti- inflammatory drug.
Vinodkumar R. Patela,
Hemant T. desaib
Research Scholar of CMJ University, Shilong, Meghalaya.
GM (Operations), Nirma Limited(Healthcare Division), Sachana, ahmedabad-380009
Abstract An optimized process developed for the synthesis of 7-ethyltryptophol, a key starting material for
etodolac, a non steroidal anti- inflammatory drug. Starting from commercially available 2-
ethylphenylhydrazine. HCl and dihydro furan with con. H2SO4 as a catalyst in N, N- dimethyl acetamide (
DMAc). H2O (1:1) as a solvent in 75% yield . the method is easy, inexpensive , without purification getting pure
solid. The process is very clean, high yielding & high quality and operationally simple.
Keywords: Etodolac, 7-ethyl tryptophol, 2-ethyl phenyl hydrazine hydrochloride, N,N-dimethyl acetamide.
I. Introduction
Tryptophol is a chemical compound that induces sleep in humans1
. It is formed in the liver after
disulfiram treatment. It is also produced by the trypanosomal parasite in sleeping sickness.tryptophol are
derivatives of indole class which contain a C-3 hydroxyethyl chain1, 2
. Tryptophol and its derivatives are
communally extracted from various natural soures3
. Some of the tryptophol derivatives exhibit biological
activity4
. Here 7-ethyl tryptophol is one of the important chemical moiety and it has a also pharmaceutical
importance.7-ethyl tryptophol is prepare from 2-ethylphenyl hydrazine hydrochloride. 7-ethyl tryptophol mainly
used for the synthesis of Etodolac5
.
Etodolac is a nonsteroidal anti-inflammatory drug (NSAID) 6
. The U.S. Food and Drug Administration
approved etodolac in January 1991. Etodolac is a non-steroidal anti-inflammatory drug (NSAID) with anti-
inflammatory, analgesic and antipyretic properties. Its therapeutic effects are due to its ability to inhibit
prostaglandin synthesis. It is indicated for relief of signs and symptoms of rheumatoid arthritis and
osteoarthritis7
. A recent clinical trial demonstrated that etodolac was effective in improving rear limb function in
dogs with chronic osteoarthritis secondary to hip dysplasia8
.
7-ethyl tryptophol chemically designated as 2-(7-ethyl – 1H-indole-3-yl) ethanol, is the key
intermediate for the preparation of Etodolac. But here we are prepare 7-ethyl tryptophol from 2-ethylphenyl
hydrazine hydrochloride with improve the yield and quality. So we are getting better yield and quality in
preparation of 7-ethyl tryptophol. The 7-ethyl tryptophol preparation has been reported by two methods. One of
the reaction of 2-ethylaniline with 2, 2, 2- trichloroethane-1, 1- diol gave the corresponding aldehyde which on
further treatment with hydroxylamine hydrochloride obtained 7-ethylisatin. This intermediate is elaborated to
final product, 7-ethyl tryptophol in three steps via 7-ethyl-3-indolylglyoxylate. The second method is Fischer
indole synthesis of 2-ethylphenylhydrazine hydrochloride and 2, 3 dihydrofuran. The later synthetic approach
reported for 7-ethyl tryptophol preparation generally carried out in water miscible solvent such as 1, 4 dioxane ,
THF , Etahnol, glyme , diglyme9,10
. These reactions are generally handled at reflux temp. so yield & quality both
are not increase and so after all getting crude 7-ethyltryptophol is purified and we are loss another yield in this
process. So while preparing the tiltle compound by the reported process e observed the inconsistency in the
process, low purity and low yield, formation of various impurities in reaction mass, lengthy workup and
difficulty in isolation.
II. Result and Discussion
As a part of our research involving synthetic process of 7-ethyl tryptophol improving method for a key
intermediate of etodolac.
In our study the reaction of 2-ethylphenyl hydrazine hydrochloride with 2, 3 dihydrofuran was tested
with different acid catalyst such as a PTSA, PPTSA, CH3COOH, and Conc. H2SO4 at 50°C for 3-4 hrs. (Table-
1)
2. A optimized process for the synthesis of a key starting material for etodolac, a non steroidal anti-
www.iosrjournals.org 4 | Page
OH
H
N
Tryptophol
N
H
OH
7-Ethyltyrptophol
HN NH2
H Cl
2-ethylphenyl hydrazine hydrochloride
N
H
O
HO
O
Etodolac
Figure 1- chemical structures of tryptophol, 7-ethyl tryptophol, 2-ethylphenyl hydrazine hydrochloride and
Etodolac.
Table-1 Reaction of 2-ethylphenyl hydrazine hydrochloride with 2, 3 dihydrofuran in the presence of various
acid catalysts at 50°C.
Sr. no. Catalyst Conversion by
HPLC(%)
1 Conc. HCl 42%
2 Con.H2SO4 80%
3 CH3COOH 45%
4 Trifflic acid 58%
5 PTSA 68%
6 PPTSA 69%
It was found that H2SO4 was superior to all the other catalyst examined and gave a good reaction conversion.
During all reactions while preparing 7-ethyltryptophol, formation of a major product was observed (42-80% by
HPLC). After completion the reaction we found that at 4.5 to 5 pH impurity not extacted in MDC. At Highly
acidic pH, Yield and purity was low and at neutral pH yield was good but purity was low.
A reaction scheme of 7-ethyl tryptophol shown in scheme-1. First we prepared hydrazone and then cyclized it
by Conc. H2SO4. The reaction of 2-ethyl phenyl hydrazine hydrochloride and 2, 3 dihydrofuran under the
present reaction conditions afforded75% yield of the 7-etyhltryptophol.
In summary, a simple and general method for the synthesis of 7-ethyltryptophol at 45°C, which offers several
advantages including good yield has been developed.
Scheme-1
NHNH2.HCl
+
O
2,3dihydrofuran
DMAc
H2O
N
H
OH
7-ethyltryptophol2-ethylphenyl hydrazine.HCl
Table-2 Effect of solvent on the reaction of 2-ethylphenyl hydrazine hydrochloride with 2, 3 dihydrofuran in the
presence of Conc. H2SO4 at 40-45°C.
Sr.no. solvent Conversion
by HPLC(%)
Yield (%)
1 H2O : CH3CN (1:1) 60.43 42
2 H2O : THF (1:1) 62.23 50
3 H2O : Ethanol (1:1) 70.99 48
4 H2O : DMAc (1:1) 86.94 80
5 H2O : IPA (1:1) 73.88 58
6 H2O : Methanol (1:1) 84.2 52
3. A optimized process for the synthesis of a key starting material for etodolac, a non steroidal anti-
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Experimental section
Melting points were determined on Buchi 540 melting point apparatus and are uncorrected. FT-IR
spectra were recorded as KBr pellet on Nicolet 380 FT –IR instrument (model thermo electron corporation
spectrum one), 1H and 13C CMR (proton decoupled) spectra were recorded on Varian 400 MHz spectrometer
using DMSO-d6, and tetramethylsilane (TMS) as internal standard. Mass spectra were recorded on Agilent
triple quadruple mass spectrometer equipped with turbo ion spray interface at 375°C.
Preparation of 7-ethyl tryptophol,
To a stirred solution of 2-ethylphenyl hydrazine hydrochloride(100gm) and DMAc-H2O (800ml),
dropwise added 2,3 dihydrofuran(40.7gm) at 25-30°C.heat the reaction mass up to 50°C and stirred for 30
mins.The completion of reaction was monitored by TLC. (TLC system: toluene: ethyl acetate 2:8) Added Conc.
H2SO4 () at 50°C and maintain the reaction mass for 3-4 hrs at same temp. The completion of reaction was
monitored by TLC. (TLC system: toluene: ethyl acetate 2:8). After completion of the reaction, reaction mixture
was allowed to cool to RT. Adjust the pH of reaction mass 4-5 by using Na2CO3 solution and then extracted
with MDC (3×700ml). The combined organic layer was washed with dil. HCl solution, then washed with
saturated bicarbonate solution and then washed with water. Dried over anhydrous sodium sulphate and
concentrated under reduced pressure below 30°C gave crude compound. Washed the residue with
cyclohexane(100ml). Dissolved the residue in Diiso propyl ether and passed the solution over the silicagel.
Distilled out the organic layer and cooled the semisolid light yellow colour product. After cooling material was
solid light yellow powder. (88 gm), yield: 80%, mp 43-45°C, HPLC Purity: NLT 95%. 1H NMR (CDCl3): δ
1.40(t,3H), 1.70(s,1H,OH), 2.90 (q,2H), 3.09(t,2H), 3.96(t,2H) ,7.14(m,3H), 7.53 (d,1H), 8.09 (broad s, 1H,
NH) , 13C NMR (CDCl3) : δ 13.85, 24.03,
28.88,62.62,112.68,116.60,119.82,120.76,122.20,126.68,127.15,135.32; ESI- MS : m/z (m+ -1) 190.15, IR
(KBR) : 3412,2958,2725,1897,1496,1433,1357,1222,1051,748 cm-1
Acknowledgement
The authors thank Dr. hemant desai sir for the provide best guidance and encourangement.
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