THE EFFECT OF ARYL FLUORINES IN A LIPASE RESOLUTION

被引：8

作者：

DASARADHI, L ^{[1
]}

OHAGAN, D ^{[1
]}

机构：

[1] UNIV DURHAM,DEPT CHEM,SCI LABS,SOUTH RD,DURHAM DH1 3LE,ENGLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(00)80036-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The steric influence of fluorine compared to hydrogen in enzymatic systems is probed by the resolution of a series of fluorinated benzhydrol acetates with lipases. Lipase AY-Amano-30 from Candida cylindracea can distinguish a single fluorine atom and the discrimination is most significant with fluorine in the ortho position close to the reaction centre. Increasing the number of fluorine atoms improves the discrimination and 2,3,4,5,6-pentafluoroaryl benzhydrol was resolved in 86%ee after 35% conversion.

引用

页码：1655 / 1658

页数：4

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