SYNTHESIS OF OXYGEN-BRIDGED ANTIGESTAGENS

被引：4

作者：

CLEVE, A

OTTOW, E

NEEF, G

WIECHERT, R

机构：

[1] Research Laboratories, Schering AG

来源：

TETRAHEDRON | 1993年 / 49卷 / 11期

关键词：

ANTIGESTAGENS; 11-BETA-SUBSTITUTED STEROIDS; 10,11-BETA-(OXY-1,2-PHENYLENE)-STEROIDS; ACID CATALYZED INTRAMOLECULAR EPOXIDE OPENING;

D O I：

10.1016/S0040-4020(01)80365-3

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A synthetic access to 10,11beta-(oxy-1,2-phenylene)-steroids 13 is described. Key steps are the S(N)2' type introduction of suitably ortho substituted arenes into vinyl epoxide 4, and ring closure by an acid catalysed intramolecular epoxide opening with the corresponding phenol. The resulting oxygen bridged steroids 13 are transformed into pharmacologically relevant progesterone antagonists 19a-c and 20.

引用

页码：2217 / 2226

页数：10

共 17 条

[1]

ARCADI A, 1990, SYNLETT, P47

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