SYNTHESIS OF 14-BETA-H ANTIPROGESTINS

被引：19

作者：

CLEVE, A ^{[1
]}

NEEF, G ^{[1
]}

OTTOW, E ^{[1
]}

SCHOLZ, S ^{[1
]}

SCHWEDE, W ^{[1
]}

机构：

[1] SCHERING AG,RES LABS,D-13342 BERLIN,GERMANY

来源：

TETRAHEDRON | 1995年 / 51卷 / 19期

关键词：

ANTIPROGESTINS; 11-BETA-SUBSTITUTED STEROIDS; 14-BETA-CONFIGURATION; PALLADIUM-CATALYZED CROSS-COUPLING;

D O I：

10.1016/0040-4020(95)00227-Y

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

An efficient approach to 14 beta-H antiprogestins is described. The key step of the synthesis is a cleavage of 17-silyl dienol ethers 7 respectively 12, which are generated from the corresponding Delta(14)-17-ketones, with hydrogen fluoride-pyridine complex. This method gave access to 14 beta-H analogs of the 11 beta,19-bridged series (type A) as well as of the 10 beta-H,11 beta-aryl series (type B).

引用

页码：5563 / 5572

页数：10

共 18 条

[1] REGIO AND STEREOSPECIFIC SYNTHESIS OF 11-BETA-SUBSTITUTED 19-NORSTEROIDS - INFLUENCE OF 11-BETA-SUBSTITUTION ON PROGESTERONE-RECEPTOR AFFINITY [J].