蛋白酶抑制剂Fosamprenavir Calcium的合成  

Synthesis of Protease Inhibitor Fosamprenavir Calcium

作　　者：胡娟[1] 肖元晶[1] 韩峰燕[1] 杨琍苹[1] 

机构地区：[1]华东师范大学化学系,上海200062

出　　处：《中国医药工业杂志》2006年第11期723-726,共4页Chinese Journal of Pharmaceuticals

摘　　要：用L-苯丙氨酸经还原、苄基化、氧化、亲核加成、催化氢化脱苄、氨基保护和环氧化制得(2S,3S)-N-叔丁氧羰基-3-氨基-1,2-环氧-4-苯基丁烷,再经环氧开环、磺化、酰化、磷酰化、还原及成盐等反应制得蛋白酶抑制剂amprenavir的前药fosamprenavir calcium,总收率10%。Fosamprenavir calcium, a prodrug of the protease inhibitor amprenavir, was synthesized from L-phenylalanine by reduction, benzylation, oxidation, nucleophilic addition, catalytic hydrogenation, protection and epoxidation to give the key intermediate （2S,3S）-N-Boc-3-amino-1,2-epoxy-4-phenylbutane, which was subjected to ring-opening reaction, sulfonation, acylation, phosphorylation, reduction and salification with an overall yield of 10 %.

关 键 词：FOSAMPRENAVIR CALCIUM AMPRENAVIR 前药 蛋白酶抑制剂 合成 

分 类 号：R978.7[医药卫生—药品]