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

DOI: 10.1016/S0960-894X(97)10156-1

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 3113 - 3118 (1997)

Update date:2022-08-05

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Authors:

Fei, Xiang-Shu

Tian, Wei-Sheng

Chen, Qing-Yun

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Article abstract of DOI:10.1016/S0960-894X(97)10156-1

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.

Full text of DOI:10.1016/S0960-894X(97)10156-1

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