Chemo-enzymatic fluorination of unactivated organic compounds

被引：116

作者：

Rentmeister, Andrea ^{[1
]}

Arnold, Frances H. ^{[1
]}

Fasan, Rudi ^{[1
]}

机构：

[1] CALTECH, Div Chem & Chem Engn, Pasadena, CA 91125 USA

来源：

NATURE CHEMICAL BIOLOGY | 2009年 / 5卷 / 01期

基金：

美国国家卫生研究院;

关键词：

NONSTEROIDAL ANTIINFLAMMATORY DRUGS; CYTOCHROME P450BM-3; MONOOXYGENASE; METABOLISM; MOLECULES; CHEMISTRY;

D O I：

10.1038/nchembio.128

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Fluorination has gained an increasingly important role in drug discovery and development. Here we describe a versatile strategy that combines cytochrome P450-catalyzed oxygenation with deoxofluorination to achieve mono- and polyfluorination of nonreactive sites in a variety of organic scaffolds. This procedure was applied for the rapid identification of fluorinated drug derivatives with enhanced membrane permeability.

引用

页码：26 / 28

页数：3

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