Synthesis of Meiosis-Activating Sterols Containing Fluorine.
摘要:
It is documented that specific types of sterol play a major role in the resumption of meiosis in oocytes from mice in vitro. 4,4-Dimethyl-5 alpha-cholesta-8,14,24-trien-3 beta-ol (FF-MAS) isolated from human follicular fluid and 4,4-dimethyl-5 alpha-cholesta-8,24-dien-3 beta-ol (T-MAS) isolated from bull testicular tissue, have been shown to activate (promote) meiosis in vitro. In order to evaluate the biological activity and stability of such compounds, new demethylsterol derivatives have been synthesised. Using diethylaminosulfur trifluoride (DAST) it was possible to synthesise selected Delta(8), Delta(14) sterols with mono and difluoro substitution at C3.
Synthesis of Meiosis-Activating Sterols Containing Fluorine.
摘要:
It is documented that specific types of sterol play a major role in the resumption of meiosis in oocytes from mice in vitro. 4,4-Dimethyl-5 alpha-cholesta-8,14,24-trien-3 beta-ol (FF-MAS) isolated from human follicular fluid and 4,4-dimethyl-5 alpha-cholesta-8,24-dien-3 beta-ol (T-MAS) isolated from bull testicular tissue, have been shown to activate (promote) meiosis in vitro. In order to evaluate the biological activity and stability of such compounds, new demethylsterol derivatives have been synthesised. Using diethylaminosulfur trifluoride (DAST) it was possible to synthesise selected Delta(8), Delta(14) sterols with mono and difluoro substitution at C3.
UNSATURATED CHOLESTANE DERIVATIVES AND THEIR USE FOR THE PREPARATION OF MEIOSIS REGULATING MEDICAMENTS
申请人:Schering Aktiengesellschaft
公开号:EP1150993A1
公开(公告)日:2001-11-07
[EN] UNSATURATED CHOLESTANE DERIVATIVES AND THEIR USE FOR THE PREPARATION OF MEIOSIS REGULATING MEDICAMENTS<br/>[FR] DERIVES DE CHOLESTANE INSATURES ET LEUR UTILISATION POUR PREPARER DES MEDICAMENTS DESTINES A REGULER LA MEIOSE
申请人:SCHERING AG
公开号:WO2000047604A1
公开(公告)日:2000-08-17
The present invention relates to pharmaceutically active unsaturated cholestane derivatives, to pharmaceutical compositions comprising them as active substances and to the use of these novel compounds for the preparation of medicaments. More particularly it has been found that the unsaturated cholestane derivatives of the invention can be used for regulating meiosis.