首页> 外国专利> PROCESS FOR PREPARING DROSPORENONE (6BETA, 7BETA, 15 BETA, 16BETA-DIMETHYLENE-3-OXO-17ALPHA-PREGN-4-ENE-21,17-CARBOLACTONE, DRSP), AS WELL AS 7ALPHA-(3-HYDROXY-1-PROPYL)-6BETA,7BETA,15BETA,16BETA-DIMETHYLENE-5BETA- -ANDROSTAN-3BETA,5,17BETA-TRIOLE(ZK 92836) AND 6BETA,7BETA,15BETA,16BETA- -DIMETHYLENE-5BETA-HYDROXY-3-OXO-17ALPHA-ANDROSTAN-21,17-CARBOLACTONE (90965) AS INTERMEDIATES OF THIS PROCESS

PROCESS FOR PREPARING DROSPORENONE (6BETA, 7BETA, 15 BETA, 16BETA-DIMETHYLENE-3-OXO-17ALPHA-PREGN-4-ENE-21,17-CARBOLACTONE, DRSP), AS WELL AS 7ALPHA-(3-HYDROXY-1-PROPYL)-6BETA,7BETA,15BETA,16BETA-DIMETHYLENE-5BETA- -ANDROSTAN-3BETA,5,17BETA-TRIOLE(ZK 92836) AND 6BETA,7BETA,15BETA,16BETA- -DIMETHYLENE-5BETA-HYDROXY-3-OXO-17ALPHA-ANDROSTAN-21,17-CARBOLACTONE (90965) AS INTERMEDIATES OF THIS PROCESS

机译:制备屈螺酮(6BETA,7BETA,15 BETA,16BETA-二甲烯-3-OXO-17ALPHA-PREGN-4-ENE-21,17-CARBOLACTONE,DRSP)以及7ALPHA-(3-HYDROXY-1-PROPYL)的制备方法)-6BETA,7BETA,15BETA,16BETA-DIMETHYLENE-5BETA- -ANDROSTAN-3BETA,5,17BETA-TRIOLE(ZK 92836)and 6BETA,7BETA,15BETA,16BETA- -DIMETHYLENE-5BETA-HYDROXY-3-OXO-17ALPHA- ANDROSTAN-21,17-甲内酯(90965)作为该过程的中间体

摘要

In the present invention, there is disclosed a process for preparing drospirenone, 6{beta},7{beta};15{beta},16{beta}-dimethylene-3-oxo-17{alpha} {alpha}-pregn-4-ene-21,17-carbolactone identified as DRSP, by catalytic hydrogenation of 17{alpha}-(3-hydroxy-1-propinyl)-6{beta},7{beta};15{beta},16{beta}-dimethylene-5{beta}-androstane-3{beta},5,17{beta}-triol, identified as ZK 34506, further by oxidizing the obtained 17{alpha}-(3-hydroxy-1-propyl)-6{beta},7{beta};15{beta},16{beta}-dimethylene-5{beta}-androstane-3{beta},5,17{beta}-triol, identified as ZK 92836, in the presence of a ruthenium salt to form 6{beta},7{beta};15{beta},16{beta}-dimethylene-5{beta}-hydroxy-3-oxo-17{alpha}-androstane-21,17-carbolactone, identified as ZK 90965 and dehydrating the latter. Disclosed is also 6{beta},7{beta};15{beta},16{beta}-dimethylene-5{beta}-hydroxy-3-oxo-17{alpha}-androstane-21,17-carbolactone as intermediate used in the above-described preparation process.
机译:在本发明中,公开了制备屈螺酮,6β,7β,15β,16β-二亚甲基-3-氧代-17α-α-孕烯丙基的方法。通过对17 {α}-(3-羟基-1-丙酰基)-6 {beta},7 {beta}; 15 {beta},16 {beta的催化氢化,鉴定为DRSP的4-ene-21,17-carbolactone }-二亚甲基-5 {beta}-雄甾烷-3 {beta},5,17 {beta}-三醇,标识为ZK 34506,进一步通过氧化获得的17 {α}-(3-羟基-1-丙基)- 6 {beta},7 {beta}; 15 {beta},16 {beta}-二亚甲基-5 {beta} -androstane-3 {beta},5,17 {beta}-三醇,在ZK 92836中钌盐的存在以形成6 {beta},7 {beta}; 15 {beta},16 {beta}-二亚甲基-5 {beta}-羟基-3-氧代17 {alpha} -androstane-21,17 -碳内酯,标识为ZK 90965并使其脱水。还公开了作为中间体的6 {beta},7 {beta}; 15 {beta},16 {beta}-二亚甲基-5 {beta}-羟基-3-氧代-17 {α}-雄甾烷-21,17-碳内酯。在上述制备过程中使用。

著录项

  • 公开/公告号CZ9900470A3

    专利类型

  • 公开/公告日1999-05-12

    原文格式PDF

  • 申请/专利权人 SCHERING AKTIENGESELLSCHAFT;

    申请/专利号CZ19990000470

  • 发明设计人 MOHR JORG-THORSTEN;NICKISCH KLAUS;

    申请日1997-08-11

  • 分类号C07J53/00;

  • 国家 CZ

  • 入库时间 2022-08-22 02:27:46

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