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Dicarbonyl compds and 21-alkanoyl-pregna- - 4-ene-3, 20-diones prepn

机译:二羰基化合物和21-烷酰基-孕烷--4-ene-3、20-二酮

摘要

Dicarbonyl compds and 21-alkanoyl-pregna-4-ene-3,20-diones prepn. Compds (I): (where R' is R1CO or CM; R" is R2CO R3OCO or CM; R1R2 and R4-R8 are H or organic residues; R3 is an organic residue; one or more of R1R2 and R4-R8 may be linked to form a cyclic residue 4C and n, and R2 are 0, 1 or 2) are prepd. simply and in good yield by treating a compd. (II) with a stony base and opt. a thiophilic agent esp. a trivalent P-compd. Prefd., products are steroids and esp. compd (III) (which are anti-inflammatory agents) and their 1,2-satd. nor derivs and DELTA, 135 (10)-triene steroids carrying a (III) 3-free, etherified or esterified OH and where R1 is an opt substd hydrocarbon; R2 is H, OH or OAcyl; R3 is H, OH, OAcyl or Me; R2 + R3 may be a bond or alkylene- or cycloalkylene-dioxy; R4 is H, Cl, OH or OAcyl; R4 + R5 may be O; R6 is Ha Hal; R4 + R6 may be a hond or epoxy; R7 is H, Me or Ha and R8 is H or when 1,2 is present H or Cl.
机译:二羰基化合物和21-烷酰基-pregna-4-ene-3,20-二酮制备。化合物(I):(其中R'为R 1 CO或CM; R”为R 2 CO,R 3 OCO或CM; R 1 R 2和R 4 -R 8为H或有机残基; R 3为有机残基; R 1 R 2和R 4 -R 8中的一个或多个可以为:连接以形成环状残基> 4C且n和R2为0、1或2)制备简单,收率高,方法是用石碱处理化合物(II),然后选择亲硫试剂,尤其是三价P-compd。Prefd。的产品为类固醇和尤其是化合物(III)(它们是抗炎药)及其1,2-饱和或衍生品和DELTA,135(10)-带有(III)的三烯类固醇3无,醚化或酯化的OH,其中R1是优选的烃基; R2是H,OH或OAcyl; R3是H,OH,OAcyl或Me; R2 + R3可以是键或亚烷基或亚环烷基二氧基; R4为H,Cl,OH或OAcyl; R4 + R5可以为O; R6为Ha Hal; R4 + R6可以为Hond或环氧; R7为H,Me或Ha且R8为H或存在1,2 H或Cl。

著录项

  • 公开/公告号CH555791A

    专利类型

  • 公开/公告日1974-11-15

    原文格式PDF

  • 申请/专利权人 CIBA-GEIGY AG;

    申请/专利号CH19690014117

  • 发明设计人

    申请日1969-09-18

  • 分类号C07C11/12;

  • 国家 CH

  • 入库时间 2022-08-23 04:08:18

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