1-(叠氮甲基)-3-溴苯置于potassium Phosphate Monohydrate,四丁基溴化铵体系中,用 水 作为反应溶剂,化学反应 4.0H,以69%的收率获得产物间溴苯甲腈 参考文献:A Green And Efficient Access To Aryl Nitriles Via An Electrochemical Anodic Oxidation 标题:A Green And Efficient Access To Aryl Nitriles Via An Electrochemical Anodic Oxidation 摘要:The Nitrile Functionality Is A Key Building Block In Synthetic Chemistry,And Has Wide Applications In Pharmaceuticals. However,Traditional Methodologies For The Synthesis Of Nitriles Are Limited To Harsh Reaction Conditions. Herein,We Report A New And Efficient Access To Aryl Nitriles By An Electrochemical Synthesis. Compared With The Conventional Synthetic Methods,This Electrochemical Synthesis Is More Environmentally Friendly And Easier To Handle. (C) 2014 Zheng-Gen Zha And Zhi-Yong Wang. Published By Elsevier B.V. On Behalf Of Chinese Chemical Society. All Rights Reserved. DOI:10.1016/j.Cclet.2014.04.024
专利号:EP-1058678-B1 优先权日:1998-02-26 标 题:Metal-catalyzed arylations and vinylations of hydrazines, hydrazones, hydroxylamines and oximes 发明人:BUCHWALD STEPHEN L; WAGAW SEBLE; GEIS OLIVER 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:A method is provided for the transition metal-catalyzed arylation, or vinylation, of hydrazines, hydrazones, and the like. Additionally, the invention provides a conceptually novel strategy, the cornerstone of which is the transition metal-catalyzed arylation or vinylation method, for the synthesis of indoles, carbazoles, and the like. The methods and strategies of the invention may be utilized in standard, parallel, and combinatorial synthetic protocols.
专利号:US-5130439-A 优先权日:1991-11-18 标题:Tetrazolylphenylboronic acid intermediates for the synthesis of AII receptor antagonists 发明人:LO YOUNG S; ROSSANO LUCIUS T 权利人:LO YOUNG S; ROSSANO LUCIUS T 摘要:Novel tetrazolylphenylboronic acids, methods for their preparation, and their use in the syntheses of angiotensin II receptor antagonists are disclosed.
专利号:US-4536599-A 优先权日:1978-08-22 标题:Synthesis of amine derivatives 发明人:MASUKO FUJIO; KATSURA TADASHI 权利人:SUMITOMO CHEMICAL CO 摘要:An amine of the formula, ##STR1## wherein R 1 , R 2 , R 3 , R 4 and R 5 are each hydrogen, alkyl or the like and n is 1, 2 or 3, including α-phenyl-β-(p-tolyl)-ethylamine, which is useful as an optically resolving agent, an intermediate of medicines and the like, is effectively produced by a novel process comprising hydrolysis of the corresponding nitrile of the formula, ##STR2## wherein R 1 , R 2 , R 3 , R 4 , R 5 and n are the same as above, followed by alkali-decomposition of the resulting amide of the formula, ##STR3## wherein R 1 , R 2 , R 3 , R 4 , R 5 and n are the same as above. An amide including the above one is effectively produced by hydrolysis of the corresponding nitrile in the presence of a base and hydrogen peroxide using an organic quaternary ammonium salt and/or a tertiary amine as a catalyst.
专利号:US-7951827-B2 优先权日:2005-05-05 标 题:Synthesis and antiprotozoal activity of dicationic 3,5-diphenylisoxazoles 发明人:TIDWELL RICHARD R; BAKUNOVA SVETLANA M; BAKUNOV STANISLAV; PATRICK DONALD A 权利人:UNIV NORTH CAROLINA 摘要:Novel dicationic 3,5-diphenylisoxazole compounds are described. Synthetic routes to these novel compounds are provided. Several of the compounds displayed in vitro activity versus Trypanosoma brucei brucei and Plasmodium falciparum comparable to that of furamidine. A majority of the novel compounds also were less toxic to VERO cells than furamidine.
专利号:US-7754188-B2 优先权日:2003-06-30 标 题:Radiolabeled cannabinoid-1 receptor modulators 发明人:BURNS H DONALD; CHEN ALEX M; GIBSON RAYMOND E; GOULET MARK T; HAGMANN WILLIAM K; HAMILL TERENCE G; JEWELL JAMES P; LIN LINUS S; LIU PING; PERESYPKIN ANDREY V 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to particular radiolabeled Cannabinoid-1 (CB1) receptor modulators, and methods of using these modulators for labeling and diagnostic imaging of Cannabinoid-1 receptors in mammals, particularly humans. In addition, intermediates useful for the synthesis of the radiolabeled Cannabinoid-1 receptor modulators are also disclosed, as well as the processes for synthesizing the radiolabeled Cannabinoid-1 receptor modulators. Still further, formulations of the radiolabeled Cannabinoid-1 receptor compounds are described.
专利号:US-7888394-B2 优先权日:2006-08-21 标 题:Synthesis, polymorphs, and pharmaceutical formulation of FAAH inhibitors 发明人:PUTMAN DAVID; DASSE OLIVIER 权利人:ORGANON NV 摘要:Pharmacological inhibition of fatty acid amide hydrolase (FAAH) activity leads to increased levels of fatty acid amides. The alkylcarbamic acid aryl ester of Formula (I), KDS-4103, is a FAAH inhibitor. Described herein is a process for the preparation of the compound of Formula (I), characterization of polymorphs of the FAAH inhibitor, and their uses therof.