血管紧张素转化酶抑制剂阿拉普利的合成研究  

Synthesis of Alacepril as an Angiotensin Transferase Inhibitor

作　　者：于慧[1] 关筱微[1] 王琳[1] 沙鑫[1] 刘晓平[1] 胡春[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《精细化工中间体》2014年第4期40-42,51,共4页Fine Chemical Intermediates

基　　金：国家自然科学基金资助项目(21072130)

摘　　要：研究了血管紧张素转化酶抑制剂阿拉普利(Alacepril)的合成新方法,以硫代乙酸、2-甲基丙烯酸为原料经过1,4-亲核加成、氯化、氨解、成盐、酯化、水解等反应合成了阿拉普利,总收率为18%。在该合成工艺中,未将L-脯氨酸的氨基进行保护,使反应步骤更简便,更适宜工业化。As an angiotensin transferase inhibitor, alacepril was synthesized in a novel way from thioacetic acid and 2-methyl acrylic acid via several reaction steps in overall yield of 18%. Compared to the literature reported process, the amino group of the L-proline used herein was not protected. This new procedure is suitable for industrial preparation with less reaction steps and convenient operation.

关 键 词：阿拉普利 持续性血管紧张素转化酶(ACE)抑制剂 2-甲基丙烯酸 

分 类 号：R972.4[医药卫生—药品]