| 蛋白酶抑制剂Fosamprenavir Calcium的合成 |
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| 引用本文： | 胡娟,肖元晶,韩峰燕,杨琍苹. 蛋白酶抑制剂Fosamprenavir Calcium的合成[J]. 中国医药工业杂志, 2006, 37(11): 723-726 |
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| 作者姓名： | 胡娟 肖元晶 韩峰燕 杨琍苹 |
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| 作者单位： | 华东师范大学化学系,上海,200062 |
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| 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％。
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| 关 键 词： | 前药 蛋白酶抑制剂 合成 |
| 文章编号： | 1001-8255（2006）11-0723-04 |
| 收稿时间： | 2006-01-16 |
| 修稿时间： | 2006-01-16 |
Synthesis of Protease Inhibitor Fosamprenavir Calcium |
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| HU Juan,XIAO Yuan-Jing,HAN Feng-Yan,YANG Li-Ping. Synthesis of Protease Inhibitor Fosamprenavir Calcium[J]. , 2006, 37(11): 723-726 |
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| Authors: | HU Juan XIAO Yuan-Jing HAN Feng-Yan YANG Li-Ping |
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| Affiliation: | Dept. of Chemistry, East China Normal University, Shanghai 200062 |
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| Abstract: | 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%. |
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| Keywords: | fosamprenavir calcium amprenavir |
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