脑啡肽酶抑制剂Acetorphan的合成  

Process for the Synthesis of Enkephalinase Inhibitor Acetorphan

作　　者：周盛峰[1] 程国侯[1] 杨凯[1] 江伟峰[1] 林盛平[1] 

机构地区：[1]华东理工大学化学与制药学院,上海200237

出　　处：《华东理工大学学报（自然科学版）》2003年第4期420-422,共3页Journal of East China University of Science and Technology

摘　　要：以苄氯和丙二酸二乙酯为起始原料,经烃化,水解,Mannich反应,脱羧和Michael加成得到2-乙酰硫甲基-3-苯基丙酸,然后与甘氨酸苄酯反应得到Acetorphan,总收率17.4%。Acetorphan, an oral enkephalinase inhibitor used in the treatment of acute diarrhoea, was synthesized from benzyl chlodride and diethyl malonate by alkylation, hydrolysis, mannich reaction, decarboxylation and Miechal addition. The 2acetylthiomethyl3phenyl propionic acid obtained reacted with glycine benzyl ester to give the desired product in an overall yield of 17.4%.

关 键 词：ACETORPHAN 脑啡肽酶抑制剂 2-乙酰硫甲基-3-苯基丙酸 

分 类 号：R9[医药卫生—药学]