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

Bioorganic & Medicinal Chemistry Letters
1997.0

Abstract

A concise synthetic approach to 4-trifluoromethyl steroids, a novel class of steroid 5α-reductase inhibitors, is described. Direct trifluoromethylation of steroid olefinic bromide with methyl fluorosulfonyldifluoroacetate was used as a key step in the synthesis. The compound 4 exhibited highly inhibitory activity than Finasteride in in vitro assay.

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