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GONA-3,5-DIENES

机译:GONA-3,5-二烯

摘要

1277759 3-Cyclopentyloxy-#SP3/SP'SP5/SP-storoids AMERICAN HOME PRODUCTS CORP 30 July 1969 [15 Oct 1968 21 April 1969 (2)] 38169/69 Heading C2U Novel steroids of the formula (wherein R is C 2-20 alkyl; RSP1/SP, RSP2/SP, RSP3/SP and RSP4/SP are each H or CH 3 ; and RSP6/SP is H or CORSP5/SP where RSP5/SP is C 1-10 alkyl, C 3-6 cycloalkyl or monocyclic aryl- C 1-6 alkyl) are prepared (1) by enol acylation of the corresponding 17#-hydroxy-#SP4/SP-3-ones followed by treatment of the products with cyclopentanol in presence of an acid catalyst to give the required steroids wherein RSP6/SP is CORSP5/SP; or (2) by enol etherification of the corresponding 17#-acyloxy-#SP4/SP-3-ones using cyclopentanol, cyclopentyl orthoformate or a dicyclopentyl ketal of a ketone in the presence of an acid catalyst, or by a similar process using as the starting material a 3-enol ester or -enol ether; or (3) by ethynylation of the corresponding 17-ones, prepared in turn from the corresponding #SP3,5/SP-3-enol esters, these being prepared by acylation of the #SP4/SP-3-ones. The products of these processes may be d-steroids or these in admixture with lsteroids e.g. racemates. The novel steroids are progestational agents and may be made up into pharmaceutical compositions with suitable carriers. They may be used, among other things, for preventing conception. Specifications 1,041,278, 1,191,347, 1,103,205 and 1,277,760 are referred to. Reference has been directed by the Comptroller to Specification 1,041,278.
机译:1277759 3-cycloopentyloxy-# 3 ' 5 -类固醇美国家用产品公司1969年7月30日[1968年10月15日(1969)(2)] 38169/69标题C2U新型类固醇式(其中R为C 2-20烷基; R 1 ,R 2 ,R 3 和R 4 分别为H或CH 3; R 6 为H或COR 5 其中R 5 为C 1-10烷基,C 3 (1)通过将相应的17#-羟基-# 4 -3-one烯醇酰化,然后用环戊醇处理产物,制备(-6环烷基或单环芳基-C 1-6烷基)(1)。在酸催化剂的存在下得到所需的甾族化合物,其中R 6 为COR 5 ;或(2)在酸催化剂的存在下,使用环戊醇,原甲酸环戊酯或酮的二环戊基缩酮对相应的17#-酰氧基-# 4 -3-进行烯醇醚化,或使用3-烯醇酯或-烯醇醚作为起始原料的类似方法;或(3)通过相应的# 3,5 -3-烯醇酯依次制备的相应的17-酮进行乙炔化,这些酯是通过## SP> 4的酰化制备的SP> -3-ones。这些过程的产物可以是d-类固醇或与类固醇混合的d-类固醇。队友。新的类固醇是孕激素,可以与合适的载体一起制成药物组合物。它们尤其可以用于防止受孕。参考规格1,041,278、1,191,347、1,103,205和1,277,760。主计长已直接参考规范1,041,278。

著录项

  • 公开/公告号GB1277759A

    专利类型

  • 公开/公告日1972-06-14

    原文格式PDF

  • 申请/专利权人 AMERICAN HOME PRODUCTS CORPORATION;

    申请/专利号GB19690038169

  • 发明设计人

    申请日1969-07-30

  • 分类号A47F3/12;A61K31/566;A61K31/567;A61K31/57;

  • 国家 GB

  • 入库时间 2022-08-23 08:06:11

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