发明名称 Process for the preparation of 1,3,5(10)-8alpha-oestratrienes
摘要 1,3,5(10)-8 alpha -oestratrienes of the following formula <IMAGE> in which R<1> is acyl and R<2> is lower alkyl are prepared. These compounds are obtained by oxidising a corresponding 3-hydroxy-13-R<2>-8 alpha -oestra-1,3,5(10)-trien-17-one with lead tetraacylate and rearranging the reaction product in the presence of a strong acid. The corresponding 1,3-hydroxy compounds are likewise prepared from the 1,3-diacyl compounds and can be converted into the corresponding diethers. The reduction of 17-keto compounds I into corresponding 17ss-hydroxy compounds is also described. The conversion of the said 17-keto compounds into 17ss-hydroxy-17 alpha R<4> compounds by reacting the 17-keto compounds with an organometallic compound which supplies the radical R<4>, which is a saturated or unsaturated, optionally substituted hydrocarbon group, is also described. The said compounds display favourable oestrogenic dissociation and can be used for the treatment of manifestations of oestrogen deficiency.
申请公布号 CH614217(A5) 申请公布日期 1979.11.15
申请号 CH19780010359 申请日期 1974.07.12
申请人 SCHERING AG 发明人 KLAUS PREZEWOWSKY;HENRY LAURENT;HELMUT HOFMEISTER;RUDOLF WIECHERT;FRIEDMUND NEUMANN;YUKISHIGE NISHINO
分类号 A61K31/565;A61P13/02;A61P15/00;C07J1/00;C07J15/00;C07J17/00;C07J31/00;C07J41/00;C07J43/00;C07J75/00;(IPC1-7):C07J1/00 主分类号 A61K31/565
代理机构 代理人
主权项
地址