首页> 外国专利> PROCESS FOR PRODUCING DROSPIRENONE (6beta, 7beta; 15beta, 16beta - DIMETHYLENE- 3-OXO-17alpha-PREGN-4-EN-21, 17-CARBOLACTONE, DRSP), AS WELL AS 7alpha- (3-HYDROXY-1-PROPYL) - 6beta, 7beta; 15beta, 16beta-DIMETHYLENE-5beta - ANDROSTANE-3beta, 5, 17beta-TRIOL (ZK 92836) AND 6beta, 7beta; 15beta, 16beta - DIMETHYLENE - 5beta HYDROXY-5-OXO-17alpha-ANDROSTANE-21,17-CARBOLACTONE

PROCESS FOR PRODUCING DROSPIRENONE (6beta, 7beta; 15beta, 16beta - DIMETHYLENE- 3-OXO-17alpha-PREGN-4-EN-21, 17-CARBOLACTONE, DRSP), AS WELL AS 7alpha- (3-HYDROXY-1-PROPYL) - 6beta, 7beta; 15beta, 16beta-DIMETHYLENE-5beta - ANDROSTANE-3beta, 5, 17beta-TRIOL (ZK 92836) AND 6beta, 7beta; 15beta, 16beta - DIMETHYLENE - 5beta HYDROXY-5-OXO-17alpha-ANDROSTANE-21,17-CARBOLACTONE

机译:制备屈螺酮(6beta,7beta; 15beta,16beta-DIMETHYLENE- 3-OXO-17alpha-PREGN-4-EN-21,17-CARBOLACTONE,DRSP)的过程以及7alpha-(3-HYDROXY-1-PROPYL) -6beta,7beta; 15beta,16beta-dimethethene-5beta-ANDROSTANE-3beta,5,17beta-TRIOL(ZK 92836)和6beta,7beta; 15beta,16beta-二甲基-5beta羟基-5-氧代-17alpha-安德鲁斯坦-21,17-碳内酯

摘要

Production of drospirenone (6beta ,7beta ;15beta ,16beta -dimethylene-3-oxo-17alpha -pregn-4-ene-21,17-carbolactone) of formula (I) comprises catalytically hydrogenating 17alpha -(3-hydroxy-1-propynyl)-6beta ,7beta ;15beta ,16beta -dimethylene-5beta -androstane-3beta ,5,17beta -triol of formula (II) to give 17alpha -(3-hydroxypropyl)-6beta ,7beta ;15beta ,16beta -dimethylene-5beta -androstane-3beta ,5,17beta -triol of formula (III), oxidising (III) in the presence of a ruthenium salt to give 6beta ,7beta ;15beta ,16beta -dimethylene-5beta -hydroxy-3-oxo-17alpha -pregnane-21,17-carbolactone of formula (IV), and dehydrating (IV): Also claimed are intermediates (III) and (IV).
机译:式(I)的屈螺酮(6β,7β;15β,16β-二亚甲基-3-氧代-17α-孕烯-4-烯-21,17-碳内酯)的生产包括催化氢化17α-(3-羟基-1-丙炔基) )-6beta,7beta; 15beta,16beta -dimethyl-5beta -androstane-3beta,5,17beta -triol的式(II),得到17alpha-(3-羟丙基)-6beta,7beta; 15beta,16beta -dimethyl-5beta-式(III)的雄烷-3β,5,17β-三醇,在钌盐的存在下氧化(III),得到6β,7β;15β,16β-二亚甲基-5β-羟基-3-氧代-17α-孕烷-式(IV)的21,17-内酯和脱水(IV):还要求保护中间体(III)和(IV)。

著录项

  • 公开/公告号IL127963A

    专利类型

  • 公开/公告日2004-06-20

    原文格式PDF

  • 申请/专利权人 SCHERING AKTIENGESELLSCHAFT;

    申请/专利号IL19970127963

  • 发明设计人

    申请日1997-08-11

  • 分类号C07J53/10;

  • 国家 IL

  • 入库时间 2022-08-21 23:10:43

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