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A practical synthesis of 3-substituted delta 3,5(6)-steroids as new potential 5 alpha-reductase inhibitor
Bioorganic & Medicinal Chemistry Letters
|January 5, 1999
Abstract:
A new and practical synthetic approach to 3-substituted delta 3,5(6)-Steroids, as potential 5 alpha-reductase inhibitor, is described. The key step involves Pd-catalyzed coupling reaction of steroid 3-enol 5H-3-oxo-octafluoropentanosulfonates. 3-Phenylacetylenyl substituted delta 3,5(6)-steroid 3g and 3-phosphate substituted delta 3,5(6)-steroid 3f in our synthesized compounds exhibited high 5 alpha-reductase inhibitory activity in vitro assay.