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Synthesis of new inhibitors of aldosterone biosynthesis

Authors
Journal
Tetrahedron
0040-4020
Publisher
Elsevier
Publication Date
Volume
44
Issue
4
Identifiers
DOI: 10.1016/s0040-4020(01)85892-0
Disciplines
  • Design

Abstract

Abstract The synthesis of 18 vinyl and 18 ethynylprogesterone 1 and 2 is described. The reported data emphasize the decisive role played by the protective group on carbon 3 in the course of reactions taking place at the angular 18 methyl group. Compounds 1 and 2 , designed as kcat inhibitors of aldosterone biosynthesis late step show substantial in vitro activity.

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