抗HIV蛋白酶抑制剂安普那韦的合成  

Synthesis and Analysis of HIV Protease Inhibitor Amprenavir

作　　者：高玲玲[1] 初秋亭[1] 王娟娟[1] 张关永[1] 

机构地区：[1]华东理工大学化学与分子工程学院,上海200237

出　　处：《化学世界》2008年第2期103-106,共4页Chemical World

摘　　要：建立了一条合成抗HIV蛋白酶抑制剂Amprenavir(安普那韦)的路线。以(2S,3R)-N-苄氧羰基-3-氨基-1-氯-4-苯基-2-丁醇为起始原料,经过环氧化、开环取代、胺的酰化、催化氢解还原、胺解等五步反应生成最终产物安普那韦。主要特点在于采用催化氢解还原法,将脱除苄氧羰基保护基和硝基还原成氨基一步完成,使工艺更简单。A synthesis method of anti-HIV protease inhibitor Amprenavir was developed.The new route starts from（2S,3R）-N-Cbz-3-amino-1-chloro-4-phenyl-butan-2-ol,and the target compound is obtained through five reactions such as epoxidation reaction,Hinsburg reaction,catalytic hydrogenolysis and ammonolysis reaction.The main point of the research is that the catalytic hydrogenolysis reaction can remove the protected group and reduce the nitro-group to amino-group at the same time to make the reaction more simple.

关 键 词：抗HIV蛋白酶抑制剂 安普那韦 催化氢解 (2S 3R)-N-苄氧羰基-3-氨基-1-氯-4-苯基-2-丁醇 

分 类 号：R914.5[医药卫生—药物化学]