Synthesis of 4-trifluoromethylsteroids:: A novel class of steroid 5α-reductase inhibitors

被引：0
|
作者：
Fei, XS [1 ]
Tian, WS [1 ]
Chen, QY [1 ]
机构：
[1] Chinese Acad Sci, Shanghai Inst Organ Chem, Lab Organofluorine Chem, Shanghai 200032, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 24期
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D O I：
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中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A concise synthetic approach to 4-trifluoromethyl steroids, a novel class of steroid 5 alpha-reductase inhibitors, is described. Direct trifluoromethylation of steroid olefinic bromide with methyl fluorosulfonyl-difluoroacetate was used as a key step in the synthesis. The compound 4 exhibited highly inhibitory activity than Finasteride in in vitro assay. (C) 1997 Elsevier Science Ltd.
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页码：3113 / 3118
页数：6
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