盐酸喹那普利的合成  

Synthesis of Quinapril Hydrochloride

作　　者：唐林生[1] 尹延柏[1] 苏明阳[1] 冯柏成[1] 

机构地区：[1]青岛科技大学化工学院,山东青岛266042

出　　处：《中国医药工业杂志》2009年第8期563-566,共4页Chinese Journal of Pharmaceuticals

摘　　要：以苯乙酮和乙醛酸为原料制得3-苯甲酰丙烯酸乙酯,与L-丙氨酸苄酯对甲苯磺酸盐经加成、酮基还原制得N-[(1S)-乙氧羰基-3-苯基丙基]-L-丙氨酸(5)。5经三光气活化后,与1,2,3,4-四氢异喹啉-3-羧酸苄酯对甲苯磺酸盐缩合,最后脱苄制得抗高血压药盐酸喹那普利,总收率约22%。Quinapril hydrochloride was synthesized from condensation of N-E （1S）-ethoxycarbonyl-3- phenylpropyl]-L-alanine （5） by activation with triphosgene, condensation with benzyl 1,2,3,4-tetrahydroisoquinoline-3- carboxylate and then debenzylation with an overall yield of about 22%. Compound 5 was prepared from acetophenone and glyoxylic acid to give ethyl 3-benzoylacrylate, which was subjected to Michael addition with L-alanine benzyl ester tosylate and then reduction.

关 键 词：喹那普利 血管紧张素转化酶抑制剂 抗高血压药 合成 

分 类 号：R972.4[医药卫生—药品]