对甲硫基苯甲腈置于盐酸,甲基锂体系中,用 四氢呋喃,乙醚,水 用作溶剂,化学反应生成4-甲硫基苯乙酮 参考文献:Method Of Treating Skin Related Conditions 标题:Method Of Treating Skin Related Conditions 摘要:一种3,4-二芳基取代噻吩类,其衍生物和类似物,包含它们的制药组合物以及使用它们治疗炎症和炎症相关疾病的方法.特别感兴趣的化合物由式i定义:其中y为s;其中x为从氢基,卤素,低烷氧基羰基和羧基中选择的一个或两个取代基;其中r2和r3分别为芳基或杂环芳基;其中r2和r3可以选择地用来自磺酰胺基,烷基磺酰基,卤素,低烷氧基和低烷基的一个或多个基团取代;或其药学上可接受的盐.
专利号:US-5786515-A 优先权日:1995-09-15 标题 :Synthesis of α-chloro or fluoro ketones 发明人:DOLLING ULF H; FREY LISA F; TILLYER RICHARD D; TSCHAEN DAVID M 权利人:MERCK & CO INC 摘要:A simple, high yielding synthesis of a-chloro ketones is described, involving acylation of Grignard and organolithium reagents with N-methoxy-N-methylchloroacetamide. The efficiency of the process is further enhanced by recycling N,O-dimethylhydroxylamine.
专利号:US-6413957-B1 优先权日:1998-04-21 标题:Methods of inhibiting cell proliferation using indeno [1,2-c]pyrazol-4-ones 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; YUE EDDY W 权利人:BRISTOL MYERS SUIBB PHARMA COM 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:US-7211598-B2 优先权日:2002-06-28 标 题:Oxime and/or hydrozone containing nitrosated and/or nitrosylated cyclooxygenase-2 selective inhibitors, compositions and methods of use 发明人:GARVEY DAVID S; RANATUNGE RAMANI R; RICHARDSON STEWART K 权利人:NITROMED INC 摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors having at least one oxime group or hydrazone group and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor having at least one oxime group or hydrazone group, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor having at least one oxime group or hydrazone group, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention having at least one oxime group or hydrazone group can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
专利号:US-7244753-B2 优先权日:2002-07-29 标 题:Cyclooxygenase-2 selective inhibitors, compositions and methods of use 发明人:GARVEY DAVID S; KHANAPURE SUBHASH P; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D 权利人:NITROMED INC 摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
专利号:US-7442802-B2 优先权日:2002-06-27 标 题:Cyclooxygenase-2 selective inhibitors, compositions and methods of use 发明人:BANDARAGE UPUL K; EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; KHANAPURE SUBHASH P; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
专利号:US-5684195-A 优先权日:1994-07-14 标 题:Method of preparing sulfmonamides from sulfones 发明人:HUANG HORNG-CHIH; HARRING SCOTT R 权利人:SEARLE & CO 摘要:A one-pot synthesis of sulfonamides from sulfones has been developed. Conversion of sulfones to the corresponding sulfinic acid salts is followed by oxidative-amination to give the sulfonamides.
参考标题:Iron-Catalyzed Synthesis Of 2H-Imidazoles From Oxime Acetates And Vinyl Azides Under Redox-Neutral Conditions 作者:Zhongzhi Zhu,Xiaodong Tang,Jianxiao Li,Xianwei Li,Wanqing Wu,Guohua Deng,Huanfeng Jiang |发布日期:2017.3.17 摘要:A Novel And Versatile Method For The Synthesis Of 2H-Imidazoles Via Iron-Catalyzed [3 + 2] Annulation From Readily Available Oxime Acetates With Vinyl Azides Has Been Developed. This Denitrogenative Process Involved N-O/n-N Bond Cleavages And Two C-N Bond Formations To Furnish 2,4-Substituted 2H-Imidazoles. This Protocol Was Performed Under Mild Reaction Conditions And Needed No Additives Or Ligands
合成参考文献
摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 348. 摘要:Lindh, J.; Larhed, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 273. 摘要:Kaneda, K.; Mitsudome, T., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2017) 1, 339. 摘要:Kaneda, K.; Mitsudome, T., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2017) 1, 344. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).