发明授权
US4089852A Process for the preparation of 21-hydroxy-16-pregnen-20-one derivatives
失效
制备21-羟基-16-孕烯-20-酮衍生物的方法
- 专利标题： Process for the preparation of 21-hydroxy-16-pregnen-20-one derivatives
- 专利标题（中）： 制备21-羟基-16-孕烯-20-酮衍生物的方法
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申请号： US682967申请日： 1976-05-04
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公开(公告)号： US4089852A公开(公告)日： 1978-05-16
- 发明人: Robert Nickolson
- 申请人： Robert Nickolson
- 申请人地址： DT Berlin and Bergkamen
- 专利权人： Schering Aktiengesellschaft
- 当前专利权人： Schering Aktiengesellschaft
- 当前专利权人地址： DT Berlin and Bergkamen
- 优先权： DT2521231 19750509
- 主分类号： C07J1/00
- IPC分类号： C07J1/00 ; C07J13/00 ; C07J17/00
摘要：
.DELTA..sup.16 -21-HYDROXY-20-KETO STEROIDS OF THE PREGNANE SERIES HAVING AN OTHERWISE UNSUBSTITUTED D-ring and a 13-methyl or -ethyl group, and 21-ethers and -esters thereof, are produced by reaction of a corresponding D-ring saturated 17-keto steroid with a lithium compound of the formula ##STR1## thereby converting the 17-keto group to a 17.beta.-hydroxy-20.alpha.-enol ether in which the 17.alpha.-side chain has the formula ##STR2## wherein R.sub.3 and R.sub.4 have the values given above, and, in any desired sequence, splitting off R.sub.3 and/or R.sub.4 enol ether by hydrolysis; eliminating 17.beta.-hydroxy group, preferably after acylation, with formation of a .DELTA..sup.16 -double bond; and, if desired, splitting off any blocking group.