首页> 外国专利> 15BETA,16BETA-METHYLENE-17ALPHA,21-DIHYDROXYPREGN-4-ENE-3,20-DIONES,THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

15BETA,16BETA-METHYLENE-17ALPHA,21-DIHYDROXYPREGN-4-ENE-3,20-DIONES,THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

机译:15BETA,16BETA-亚甲基-17ALPHA,21-二羟基-4-4-3,20-二酮,其制备及组成它们的药物成分

摘要

Trihydroxypregnene-3,20-diones (I) and especially 11 beta, 17 alpha, 21-trihydroxy-15, 16 beta-methylene-pregnene (4)-(and pregna-1,4-diene)-3,20-dione, for use as anti-inflammatories. R6 and R9 independently are H, halogen, R17, R21 independently are OH or O-acyl; Z is CO or beta-CH2OH. Preparation of (I) and 1,2-dehydro-deriv. by numerous methods e.g. (a) microbiological 11-hydroxylation of (I) (Z=CH2); (b) 1,2-dehydrogenation of a cmpd. (I); (c) adding HOCl or HOBr to the 9,11-double bond a cmpd. (I) or its, 1,2-dehydro-derivs. (Z = HC). In an example 11 beta, 17 alpha-21-trihydroxy-15,16 beta-methylene-pregnene (4)-3,20-dione, m.p. 219-221 degrees is obtained by microbiological hydroxylation of 17 alpha, 21-dihydroxy-15,16 beta-methylene-pregnene (4)-3,20-dione using Coniothyrium hellebori as organism.
机译:三羟基孕烯-3,20-二酮(I),尤其是11β,17α,21-三羟基15、16β-亚甲基-孕烯(4)-(和pregna-1,4-二烯)-3,20-二酮,用作抗炎药。 R6和R9独立地是H,卤素,R17,R21独立地是OH或O-酰基; Z是CO或β-CH2 OH。 (I)和1,2-脱氢衍生物的制备。通过多种方法(a)(I)(Z = CH2)的微生物11-羟基化; (b)cmpd的1,2-脱氢。 (一世); (c)在cmpd的9,11-双键中加入HOCl或HOBr。 (I)或其1,2-脱氢衍生物。 (Z = HC)。在一个实例中,11β,17α-21-三羟基-15,16β-亚甲基-孕烯(4)-3,20-二酮,m.p。 219-221度是通过使用黑夜蛾(Coniothyrium hellebori)作为生物体对17α,21-二羟基-15,16β-亚甲基-孕烯(4)-3,20-二酮进行微生物羟基化获得的。

著录项

  • 公开/公告号IL35790A

    专利类型

  • 公开/公告日1974-05-16

    原文格式PDF

  • 申请/专利权人 SPARAMEDICA AG;

    申请/专利号IL19700035790

  • 发明设计人

    申请日1970-12-04

  • 分类号A61K17/00;C07C171/00;

  • 国家 IL

  • 入库时间 2022-08-23 06:11:00

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