| 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 |
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| 引用本文： | Kafssi Hassan,王涛,万平玉,侯玉庆. 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[J]. 化学试剂, 2007, 29(6): 371-372,375 |
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| 作者姓名： | Kafssi Hassan 王涛 万平玉 侯玉庆 |
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| 作者单位： | 北京化工大学,化学系,北京,100029;北京化工大学,化学系,北京,100029;北京化工大学,化学系,北京,100029;北京化工大学,化学系,北京,100029 |
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| 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。
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| 关 键 词： | 盐酸贝那普利 中间体 制备 |
| 文章编号： | 0258-3283（2007）06-0371-02 |
| 修稿时间： | 2006-12-07 |
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 |
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| KAFSSI Hassan,WANG Tao,WAN Ping-yu,HOU Yu-qing. 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[J]. Chemical Reagents, 2007, 29(6): 371-372,375 |
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| Authors: | KAFSSI Hassan WANG Tao WAN Ping-yu HOU Yu-qing |
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| Affiliation: | Department of Chemistry, Beijing University of Chemical Technology, Beijing 100029, China |
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| Abstract: | 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 benazepril 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. |
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| Keywords: | benazepril hydrochloride intermediate preparation |
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