TOTAL SYNTHESIS OF ANTITUMOR AGENT AT-125, (ALPHA-S,5S)-ALPHA-AMINO-3-CHLORO-4,5-DIHYDRO-5-ISOXAZOLEACETIC ACID

被引：35

作者：

BALDWIN, JE ^{[1
]}

CHA, JK ^{[1
]}

KRUSE, LI ^{[1
]}

机构：

[1] DYSON PERRINS LAB, OXFORD OX1 3QY, ENGLAND

来源：

TETRAHEDRON | 1985年 / 41卷 / 22期

关键词：

D O I：

10.1016/S0040-4020(01)96774-2

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A short and efficient total synthesis of racemic AT-125 and its racemic threo isomer proceeds via an intramolecular Michael cyclization of a protected .alpha.,.beta.-dehydroglutamic acid .gamma.-hydroxamate. Separation of diastereomers and deprotection to racemic AT-125 followed by enzymatic resolution of the N-chloroacetamide with hog-kidney acylase provides the natural .alpha.S,5S isomer.

引用

页码：5241 / 5260

页数：20

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