专利号:US-7138526-B1 优先权日:1999-06-15 标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives 发明人:HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M 权利人:AVENTIS PHARMA INC 摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
专利号:US-9085538-B2 优先权日:2010-07-26 标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof 发明人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO 权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS 摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
专利号:US-10040752-B2 优先权日:2015-08-24 标 题 :Synthesis of levomethadone hydrochloride or dextromethadone hydrochloride and methods for use thereof 发明人:MKRTCHYAN GNEL; YAO QINGWEI 权利人:CODY LABORATORIES INC 摘要:Highly efficient methods for synthesis of levomethadone hydrochloride or dextromethadone hydrochloride are provided starting from D-alanine, or L-alanine, respectively, with retention of configuration. Methods for treating a subject are provided comprising administering a composition comprising an effective amount of levomethadone hydrochloride having not more than 10 ppm dextromethadone.
专利号:US-4284582-A 优先权日:1978-04-28 标 题 :Process for the preparation of cyclopropane derivatives, intermediates in the synthesis of pyrethroid insecticides 发明人:KAYE ALBERT E; TUCKER ALAN C 权利人:ICI LTD 摘要:Compounds of formula: wherein both groups X are chlorine, bromine or trifluoromethyl, or one X is chlorine or bromine and the other is trifluoromethyl, and Y is -CN or -COOR in which R is an alkyl group, are obtained by (A) reacting a compound of the formula: wherein X1 is chlorine or bromine, with a compound of the formula: X2C=CH-CH=C(CH3)2 in the presence of metallic copper or at least one copper salt and a base, or (B) reacting a compound of the formula: Y-CH2-CN with a compound of the formula: X2C=CH-CH=C(CH3)2 and chlorine or bromine, in the presence of at least one reducible copper salt and a base, or (C) reacting a compound of formula: X-CH2-CN with a compound of the formula: wherein X1 is chlorine or bromine, in the presence of at least one copper salt. The compounds are intermediates in the synthesis of pyrethroid insecticides.
专利号:US-2013338369-A1 优先权日:2011-03-07 标 题 :Process for the Synthesis of Aminobiphenylene 发明人:HEINRICH MARKUS; PRATSCH GERALD 权利人:HEINRICH MARKUS; PRATSCH GERALD; BASF SE 摘要:The present invention relates to a process for the synthesis of 2-aminobiphenylene and derivatives thereof by reacting a benzene diazonium salt with an aniline compound under basic reaction conditions.
专利号:US-4749797-A 优先权日:1983-04-08 标题 :Tetra-alkyl-2,2,5,5-cyclohexanone-4-01-1 compounds and their sulphonyl derivatives, the process and the intermediates for preparing them and their use in the synthesis of cis-cyclopropane lactones 发明人:D ANGELO JEAN; REVIAL GILBERT; AZERAD ROBERT; BUISSON DIDIER 权利人:ROUSSEL UCLAF 摘要:New tetra-alkyl-2,2,5,5-cyclohexanone-4-ol-1-compounds and their sulphonyl derivatives with the general formula: ##STR1## in which: each of R and R', identical or different, represents an alkyl radical (1-5 carbons) and R' represents a hydrogen atom or a radical SO 2 R'' in which R'' represents an alkyl radical (1-5 carbons) or an aryl radical (6-14 carbons), the process and the intermediates for their preparation, as well as their use in the synthesis of cyclopropane lactones of cis structure.
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合成参考文献
参考文献:10.1021/ja205046h 摘要:Solorio-Alvarado CR, Wang Y, Echavarren AM. Cyclopropanation with gold(I) carbenes by retro-Buchner reaction from cycloheptatrienes. J Am Chem Soc. 2011 Aug 10;133(31):11952–5. doi: 10.1021/ja205046h.