专利号:US-4161609-A 优先权日:1977-09-14 标题:Synthesis of carboxylic acid esters 发明人:CRAMER RICHARD D 权利人:DU PONT 摘要:A method is provided for converting a carboxylic acid amide to a carboxylic acid ester by reacting a vaporized mixture of the amide and an aliphatic alcohol or a phenol in the presence of a suitable catalyst at temperatures of from 100 DEG C. to 400 DEG C. The process is especially useful for the conversion of methacrylamide to methyl methacrylate.
专利号:US-5021444-A 优先权日:1986-01-28 标题 :Thianaphthene derivatives 发明人:TRADA ATSUSUKE; AMEMIYA YOSHIYA; MATSUDA KEIICHI; OSHIMA TAKESHI 权利人:SANKYO CO 摘要:Compounds of formula (I): ##STR1## (wherein n is 0 or 1, R 1 and R 2 are hydrogen or alkyl, one of A 1 and A 2 is --Z--Y and the other is --W--COOH, where W and Z are alkenylene or alkylene and Y is imidazolyl or pyridyl, and the broken lines represent two single bonds or one single bond and one double bond) and their salts, esters and amides have the ability to inhibit the synthesis of thromboxane A 2 and hence are useful in the treatment of prophylaxis of thrombotic conditions. They may be prepared by introducing an imidazolyl or pyridyl group into the corresponding compound in which Y is replaced by an active group or atom.
专利号:US-2008242662-A1 优先权日:2005-05-31 标题 :Organic Compounds 发明人:NIHONYANAGI ATSUKO; TOYAO ATSUSHI; IWAKI YUKI; MASUYA KEIICHI 权利人:NIHONYANAGI ATSUKO; TOYAO ATSUSHI; IWAKI YUKI; MASUYA KEIICHI 摘要:The invention relates to substituted 3,4- or higher substituted piperazine compounds, the use thereof for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; pharmaceutical formulations or products comprising said compounds, and/or a method of treatment comprising administering said compounds, a method for the manufacture of said compounds as well as novel intermediates, starting materials and/or partial steps for their synthesis. The compounds are especially of the formula I, n n n n n n n n n n wherein R1, R2, R11, C, E and D are as defined in the specification.
专利号:US-10017481-B2 优先权日:2012-03-17 标 题 :Conformationally constrained, fully synthetic macrocyclic compounds 发明人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; PIETTRE ARNAUD; GOSALBES JEAN-FRANÇOIS; THOMMEN MARC 权利人:POLYPHOR AG 摘要:The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.
专利号:US-6465507-B2 优先权日:2000-02-28 标题 :3-(pyrolyllactone)-2-indolinone compounds as kinase inhibitors 发明人:TANG PENG CHO; MILLER TODD A; LI XIAOYUAN; ZHANG RUOFEI; CUI JINRONG; HUANG PING; WEI CHUNG CHUN 权利人:SUGEN INC 摘要:The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds of the invention. The invention also relates to methods of modulating the function of protein kinases using indolinone compounds of the invention and methods of treating diseases by modulating the function of protein kinases and related signal transduction pathways.
专利号:CN-109369555-A 优先权日:2018-11-29 标题 :A kind of method of microwave radiation benzamide compound synthesis benzoxazoles in water phase
参考标题:A Novel Oxidative Procedure For The Synthesis Of Benzamides From Styrenes And Amines Under Metal-Free Conditions 作者:Muhammad Sharif,Jin-Long Gong,Peter Langer,Matthias Beller,Xiao-Feng Wu 摘要:An Interesting Procedure For The Oxidative Synthesis Of Amides From Styrenes And Amines Has Been Developed. Various Primary Amides Were Formed In Moderate Yields (25-81%). Secondary Amides Can Be Produced In Moderate Yields As Well (41-68%). Notably, No Transition Metal Catalyst Was Needed For This Transformation. This Is The First Example Of Oxidative Transformation Of Styrenes To Benzamides.
合成参考文献
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