SYNTHESIS OF 4-TRIFLUOROMETHYLSTEROIDS - A NOVEL CLASS OF STEROID 5-ALPHA-REDUCTASE INHIBITORS

Authors
FEI XS TIAN WS CHEN QY
Citation
Xs. Fei et al., SYNTHESIS OF 4-TRIFLUOROMETHYLSTEROIDS - A NOVEL CLASS OF STEROID 5-ALPHA-REDUCTASE INHIBITORS, Bioorganic & medicinal chemistry letters, 7(24), 1997, pp. 3113-3118
Citations number
32
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
24
Year of publication
1997
Pages
3113 - 3118
Database
ISI
SICI code
0960-894X(1997)7:24<3113:SO4-AN>2.0.ZU;2-7
Abstract
A concise synthetic approach to 4-trifluoromethyl steroids, a novel cl ass of steroid 5 alpha-reductase inhibitors, is described. Direct trif luoromethylation of steroid olefinic bromide with methyl fluorosulfony l-difluoroacetate was used as a key step in the synthesis. The compoun d 4 exhibited highly inhibitory activity than Finasteride in in vitro assay. (C) 1997 Elsevier Science Ltd.