A practical synthesis of 3-substituted delta 3,5(6)-steroids as new potential 5 alpha-reductase inhibitor.
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.
Tian
W
W
Shanghai Institute of Organic Chemistry, Chinese Academy of Science, China.
Zhu
Z
Z
Liao
Q
Q
Wu
Y
Y
D058891:5-alpha Reductase Inhibitors; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013256:Steroids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D058891:5-alpha Reductase Inhibitors; D004791:Enzyme Inhibitors; D013256:Steroids