首页> 外国专利> 21-Hydroxy 4-pregnene derivs. - for arterial hypertension and cardial insufficiency are prepd. from 3-oxo 20,20-ethylene di:oxy pregnene

21-Hydroxy 4-pregnene derivs. - for arterial hypertension and cardial insufficiency are prepd. from 3-oxo 20,20-ethylene di:oxy pregnene

机译:21-羟基4-孕烯衍生。 -对于动脉高血压和心脏功能不全的患者,请做好准备。由3-氧代20,20-乙烯二:氧孕烯

摘要

3,20-dioxo-7 alpha-acetylthio-21-hydroxy pregn-4-ene (I) adn 2,2-dimethyl-3,20-dioxo-21-propionyloxy-pregn-4-ene (I:Z is H, R1 is propionyloxy) are new. In (I) Z is acetylthio; R1 is OH; and in (II) Z is H; R is propionloxy. Used in treatment of arterial hypertension and cardiac insufficiently. The cpds are aldosterone antagonists and increase Na diuresis while maintaining organic K. In an example, (I) was prepd. from 3-oxo-20, 20-ethylene dioxy pregn-4-ene by methylation (CH3I), hydrolysis of the ketal, conversion of the 4,6-diene, with dichloro dicyano benzoquinone, acetoxylation at the 21-position with Pb tetraacetate and BF3 etherate, removal of the acetyl gp., and finally treatment with thioacetate acid.
机译:3,20-二氧杂-7α-乙酰硫基-21-羟基孕烯4-烯(I)和2,2-二甲基-3,20-二氧杂-21-丙酰氧基-孕烯4-烯(I:Z为H ,R1是丙酰氧基)是新的。在(I)中,Z为乙酰硫基; R1为OH;在(II)中,Z为H; R是丙氧基。用于动脉高血压和心脏不足的治疗。 cpds是醛固酮拮抗剂,可在维持有机K的同时增加Na利尿作用。在一个实例中,制备(I)。由甲基化(CH3I)生成的3-oxo-20、20-乙烯二氧孕烯-4-烯,缩酮的水解,4,6-二烯的转化,与二氯二氰基苯并醌的反应,在21位用四乙酸铅进行乙酰化和BF 3醚化,除去乙酰基,最后用硫代乙酸处理。

著录项

  • 公开/公告号FR2362631A2

    专利类型

  • 公开/公告日1978-03-24

    原文格式PDF

  • 申请/专利权人 ROUSSEL UCLAFF;

    申请/专利号FR19760025939

  • 发明设计人

    申请日1976-08-27

  • 分类号A61K31/57;C07J5/00;

  • 国家 FR

  • 入库时间 2022-08-22 21:45:13

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