培哚普利置于叔丁胺体系中,用 乙酸乙酯 用作溶剂,化学反应 1.5H,以65%的收率获得培哚普利叔丁胺盐 参考文献:Process For The Preparation Of Perindopril 标题:Process For The Preparation Of Perindopril 摘要:提供了制备依那普利中间体的新方法.同时,还提供了改进的依那普利厄布明制备方法,包括(A)将式(15)化合物与硅烷基化的八氢吲哚-1H-2-羧酸反应以形成依那普利;以及(B)将依那普利与叔丁基胺反应以形成式i的依那普利厄布明.
专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-7323575-B2 优先权日:2003-04-09 标题:Process for the synthesis of (2S)-indoline-2-carboxylic acid 发明人:SOUVIE JEAN-CLAUDE; LECOUVE JEAN-PIERRE 权利人:SERVIER LAB 摘要:Process for the synthesis of (2S)-indoline-2-carboxylic acid of formula (I): n nApplication in the synthesis of perindopril and its pharmaceutically acceptable salts.
专利号:US-6774259-B2 优先权日:2000-04-11 标 题 :Method for synthesis of n-[(s)]-1-carboxybutyl-(s)-alanine esters and use in synthesis of perindopril 发明人:SOUVIE JEAN-CLAUDE; RENAUD ALAIN 权利人:SERVIER LAB 摘要:A stereoselective process for the industrial synthesis of compounds of formula (I):wherein R represents linear or branched (C1-C6)alkyl, andapplication in the synthesis of perindopril and pharmaceutically acceptable salts thereof.
专利号:US-6818788-B2 优先权日:2000-03-31 标 题:Method for synthesis of n-[(s)-1-carboxybutyl]-(s)-alanine esters and use in synthesis of perindopril 发明人:SOUVIE JEAN-CLAUDE 权利人:SERVIER LAB 摘要:Stereoselective process for the industrial synthesis of compounds of formula (I):wherein R represents linear or branched (C1-C6)alkyl.Application in the synthesis of perindopril and pharmaceutically acceptable salts thereof.
专利号:US-4902817-A 优先权日:1987-09-17 标 题 :Process for the synthesis of alpha n alkylated amino acids and esters thereof, application to the synthesis of carboxyalkyl dipeptides 发明人:VINCENT MICHEL; BALIARDA JEAN; MARCHAND BERNARD; REMOND GEORGES 权利人:ADIR 摘要:Stereoselective process for the industrial synthesis of compounds of formula (I): ##STR1## where R 1 is linear or branched lower alkyl with 1 to 6 carbon atoms, n R 2 is a linear or branched lower alkyl with 1 to 4 carbon atoms, n employing inexpensive starting materials and obtaining optimum yields. n Application to the synthesis of carboxyalkyl dipeptides.
专利号:US-7288661-B2 优先权日:2003-12-10 标 题 :Process for the synthesis of (2S,3aS,7aS)-1-[(S)-alanyl]-octahydro-1H-indole-2-carboxylic acid compounds and application in the synthesis of perindopril 发明人:DUBUFFET THIERRY; LECOUVE JEAN-PIERRE 权利人:SERVIER LAB 摘要:Process for the synthesis of compounds of formula (I): n nwherein R represents a hydrogen atom or a protecting group for the amino function.n n Application in the synthesis of perindopril and pharmaceutically acceptable salts thereof.
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