A practical synthesis of 3-substituted Δ3,5(6)-steroids as new potential 5α-reductase inhibitor

被引：0
|
作者：
Tian, WS
Zhu, Z
Liao, QJ
Wu, YK
机构：
[1] Chinese Acad Sci, Shanghai Inst Organ Chem, Shanghai 200032, Peoples R China
[2] Pharmaceut Univ China, Dept Med Chem, Nanjing 210009, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 15期
关键词：
5 alpha-reductase inhibitor; synthesis; coupling reaction;
D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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. (C) 1998 Elsevier Science Ltd. All rights reserved.
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页码：1949 / 1952
页数：4
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