| 盐酸咪达普利的合成 |
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| 引用本文： | 张伟杰,韦萍.盐酸咪达普利的合成[J].现代化工,2011,31(Z1). |
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| 作者姓名： | 张伟杰 韦萍 |
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| 作者单位： | 南京工业大学生物与制药工程学院,江苏南京,211800 |
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| 摘 要： | N-苄氧羰基-L-天冬酰胺经环化、酯化、甲基化,脱苄氧羰基得到关键中间体(4S)-1-甲基-2-氧代咪唑啉-4-羧酸叔丁酯.再与由N- (S) -1-乙氧羰基-3-苯丙基]-L-丙氨酸进行酰化反应,利用氯化氢脱去叔丁基,得到咪达普利盐酸盐,总收率约为26％(以N-苄氧羰基-L-天冬酰胺计).
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| 关 键 词： | 盐酸咪达普利 血管紧张素转换酶抑制剂 合成 |
Synthesis of imidapril hydrochloride |
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| ZHANG Wei-jie,WEI Ping.Synthesis of imidapril hydrochloride[J].Modern Chemical Industry,2011,31(Z1). |
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| Authors: | ZHANG Wei-jie WEI Ping |
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| Affiliation: | ZHANG Wei-jie,WEI Ping(School of Biotechnology and Pharmaceutical Engineering,Nanjing University of Technology,Nanjing 211800,China) |
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| Abstract: | N-benzyloxycarbonyl-L-asparagine underwent cyclization,esterification,methylation,De-Cbz reaction to afford the key intermediate(4S)-1-methyl-2-oxo-imidazolin-4-carboxylic acid tert-butyl,followed by acylation with N-(S)-1-ethyoxyoxo-3-phenylpropyl]-L-alanine and removal of tertbutyl group using hydrochloride gas to generate imidapril hydrochloride.The total yield is about 26%(based on N-Carbobenzyloxy-L-asparagine). |
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| Keywords: | imidapril hydrochloride angiotensin-converting enzyme inhibitors synthesis |
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