3-[(1-乙氧羰基-3-苯基丙基)氨基]-2,3,4,5-四氢-2-氧代-1-H-1-苯并氮杂卓-1-乙酸叔丁酯的制备研究  

Study on the preparation of 3-[(1-ethoxycarbonyl-3-phenylpropyl) amino]-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepine-1-acetate tert-butyl ester

作　　者：Kafssi Hassan 王涛[1] 平玉 侯玉庆[1] 

机构地区：[1]北京化工大学化学系,北京100029

出　　处：《化学试剂》2007年第6期371-372,375,共3页Chemical Reagents

摘　　要：以3-溴-2,3,4,5-四氢-1H-1-苯并氮杂卓-2-酮、L-苯并丁氨酸乙酯(LHPE)和氯乙酸叔丁酯为原料,经两次烷基化反应,合成出制备盐酸贝那普利的中间体[3-[(1-乙氧羰基-3-苯基丙基)氨基]-2,3,4,5-四氢-2-氧代-1-H-1-苯并氮杂卓-1-乙酸叔丁酯(EATOA),并考察了反应条件对收率及手性异构体比例的影响。3- [ （1-ethoxycarbonyl-3-phenylpropyl） amino]-2,3,4, 5-tetrahydro-2-oxo-1H-1-benzazepine-1-acetate tert-butyl ester is the intermediate of benazepfil hydrochloride. The present work disclosed a novel process of using L-homphenylalanine alkyl ester, tert-butyl-3-bromo-2, 3, 4, 5：tetrahydro-2-oxo-1H-benzazepine-1-acetate and 3-bromo-2, 3,4, 5-tetrahydro-2-oxo-1H-benzazepine as the starting materials for synthesis through two steps of alkylation. The effect of reaction conditions on the yield and the ratio of diastereomers were discussed.

关 键 词：盐酸贝那普利 中间体 制备 

分 类 号：H914.5[语言文字—世界语]