【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%。更多还原

【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%.更多还原