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1.
Undare Santosh S. Valekar Navnath J. Patravale Ajinkya A. Jamale Dattatraya K. Vibhute Sunil S. Walekar Laxman S. Kolekar Govind B. Deshmukh M. B. Anbhule Prashant V. 《Research on Chemical Intermediates》2016,42(5):4373-4386
Research on Chemical Intermediates - A simple methodology has been developed for the synthesis of diverse members of multifunctionalized 4-hydroxy-2-methyl-6-(phenyl)pyrimidine-5-carbonitrile... 相似文献
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Sanjay A. Jadhav Shashikant B. Landge Samadhan S. Shelke Navanath C. Niphade Raghavendra K. Panchangam Vijayavitthal T. Mathad Saroj R. Bembalkar 《Chromatographia》2010,71(11-12):1055-1061
A rapid and sensitive gas chromatographic method using flame ionization detection (GC–FID) has been developed and validated for five process related non-chromophoric impurities viz, 2-(2-chloroethoxy)ethanol (2-CEE), piperazine, 2-(piperazin-1-yl)ethanol (HEP), 2-[2-(piperazin-1-yl)ethoxy]ethanol (HEEP), 2,2-[piperazine-1,4-diylbis(ethane-2,1-diyloxy)]diethanol (DEEP) observed during the process development of quetiapine hemifumarate, an antipsychotic drug is presented. All five non-chromophoric impurities ranging from 0.05 to 0.1% were detected using DB-5 (30 m × 0.53 mm, 5 μm) column with a good peak separation. The method was fully validated according to the ICH Q2 (R1) guidelines. The investigated validation protocols showed that the method has acceptable specificity, accuracy, linearity, precision, robustness and high sensitivity with detection limits and quantitation limits ranging from 0.001 to 0.01% and 0.004 to 0.03%, respectively. These non-chromophoric impurities generated during the process were identified by GC–MS and are characterized by MS, 1H NMR and FT-IR spectroscopy. 相似文献
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Sunil Vibhute Dattatraya Jamale Santosh Undare Navanath Valekar Kirti Patil Govind Kolekar 《合成通讯》2017,47(19):1747-1757
An environmental friendly synthetic route has been investigated for the synthesis of quinazolin-8 (4H)-one derivatives in the presence of anthranilic acid as a catalyst. The zwitter ion formed in course of reaction may a play key role in the desired transformations leading good to excellent yields. Evaluation of the present protocol by green chemistry metrics demonstrated that it is highly efficient and eco-compatible. 相似文献
4.
Kulkarni RV Boppana R Krishna Mohan G Mutalik S Kalyane NV 《Journal of colloid and interface science》2012,367(1):509-517
In the present work, we synthesized pH-responsive interpenetrating network (IPN) hydrogel beads of polyacrylamide grafted κ-carrageenan (PAAm-g-CG) and sodium alginate (SA) for targeting ketoprofen to the intestine. The PAAm-g-CG was synthesized by free radical polymerization followed by alkaline hydrolysis under nitrogen gas. The PAAm-g-CG was characterized by elemental analysis, FTIR spectroscopy and thermogravimetric analysis (TGA). The drug-loaded IPN hydrogel beads were prepared by simple ionotropic gelation/covalent crosslinking method. The amorphous nature of drug in the beads was confirmed by differential scanning calorimetry and X-ray diffraction studies. The spherical shape of the beads was confirmed by scanning electron microscopic analysis. The beads exhibited ample pH-responsive behavior in the pulsatile swelling study. The ketoprofen release was significantly increased when pH of the medium was changed from acidic to alkaline. The beads showed maximum of 10% drug release in acidic medium of pH 1.2, and about 90% drug release was recorded in alkaline medium of pH 7.4. Stomach histopathology of albino rats indicated that the prepared beads were able to retard the drug release in stomach leading to the reduced ulceration, hemorrhage and erosion of gastric mucosa. 相似文献
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D. K. Jamale S. S. Vibhute S. S. Undare N. J. Valekar K. T. Patil P. P. Warekar 《合成通讯》2013,43(21):2750-2760
AbstractThe present study describes L-hydroxy proline catalyzed unpredicted formation of 4,5-dihydro-1H-pyrazolo[3,4-b]pyridines instead of expected 4,7-dihydro-1H-pyrazolo[3,4-b]pyridines in aqueous ethanol at ambient temperature through one-pot three-component reaction. Furthermore, this protocol was evaluated using green chemistry metrics indicating green relevance of the present synthetic methodology. Most of the synthesized compounds were evaluated for their antitubercular activity against Mycobacterium tuberculosis H37RV strain, showing excellent results based on minimum inhibitory concentrations (MIC). Among the screened derivatives 4f, 4i, and 4j exhibited antitubercular activity with promising MIC value of 1.6?μg/mL. 相似文献
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Dattatraya K. Jamale Santosh S. Undare Navanath J. Valekar Aniket P. Sarkate Govind B. Kolekar Prashant V. Anbhule 《Journal of heterocyclic chemistry》2019,56(2):608-618
A series of 4‐(1H‐pyrazol‐4‐yl)‐polyhydroquinolines were synthesized through one‐pot four‐component Hantzsch condensation of 1,3‐diphenyl‐1H‐pyrazole‐4‐carbaldehydes, ammonium acetate, dimedone, and alkyl acetoacetate in glycerol as a green reaction medium. The structures of the compounds are verified by spectroscopic methods and screened for their antimicrobial activity against Mycobacterium tuberculosis H37RV strain. Almost all the synthesized derivatives reveal excellent antitubercular activity based on minimum inhibitory concentration. Especially the compounds 5h and 5k exhibit outstanding antitubercular activity with minimum inhibitory concentration 1.6 μg/mL. In addition, molecular docking study of synthesized scaffolds against enoyl‐acyl carrier protein reductase from M. tuberculosis was performed to propose the binding modes. 相似文献
7.
Sequence Selective Michael Addition for Synthesis of Indeno‐Pyridine and Indeno‐Pyran Derivatives in One‐Pot Reaction Using CuO Nanoparticles in Water 下载免费PDF全文
Navanath J. Valekar Prasad P. Patil Anil H. Gore Govind B. Kolekar Madhukar B. Deshmukh Prashant V. Anbhule 《Journal of heterocyclic chemistry》2015,52(6):1669-1676
The alternate synthesis of indeno‐pyridine and indeno‐pyran derivatives have been described by an unprecedented, green, one‐pot reaction of aromatic aldehydes, malononitrile, and indane 1,3‐dione. The formation of either indeno‐pyridine or indeno‐pyran derivatives based on a precise change in the Michael addition of indane 1,3‐dione or malononitrile on Knoevenagel product during the progress of reaction has been investigated. The reaction completed up to 30 min of time using CuO nanoparticles in water at an ambient temperature renders the protocol novel and environment friendly. All the synthesized compounds have been confirmed on the basis of their spectroscopic data. The CuO nanoparticles have been prepared by coprecipitation method and characterized by SEM, PXRD spectroscopy, and UV spectroscopy. 相似文献
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Kirti T. Patil Dattatrya K. Jamale Navnath J. Valekar Priyanka T. Patil Poojali P. Warekar Govind B. Kolekar 《合成通讯》2017,47(2):111-120
Fused pyrazolopyranopyrimidines containing both biologically active pyranopyrazole and pyranopyrimidine compounds were synthesized using a one-pot, four-component reaction of ethyl aceto acetate, hydrazine hydrate, benzaldehydes, and thiobarbituric acid without catalyst in ethanol. All target compounds obtained in very good to excellent yields over short reaction times by adapting a simple workup procedure. All the synthesized compounds exhibited good to excellent antituberculosis activities. The results shown that 4-(1H-imidazol-2-yl)-3-methyl-7-thioxo-4,6,7,8-tetrahydropyrazolo[4’,3′:5,6]pyrano[2,3-d] pyrimidin-5(1H)-one (5a) is a good antitubercular agent, as good as the standard streptomycin drug, based on minimum inhibitory concentration (MIC). 相似文献
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Patil Priyanka T. Warekar Poojali P. Patil Kirti T. Undare Santosh S. Jamale D. K. Vibhute S. S. Valekar N. J. Kolekar Govind B. Deshmukh Madhukar B. Anbhule Prashant. V. 《Research on Chemical Intermediates》2018,44(2):1119-1130
Research on Chemical Intermediates - An efficient one-pot synthesis of novel pyrazolo[3,4-b][1,8]naphthyridine and pyrazolo[3,4-d]pyrimido[1,2-a]pyrimidine derivatives has been investigated from... 相似文献
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