首页> 外国专利> PROCESS FOR PREPARING 17DELTA-PROPADIENYL-ESTRA-4,9(10)-DIENE-17BETA-O1-3-ONE OR THE 17BETA-ACETOXY DERIVATIVE THEREOF

PROCESS FOR PREPARING 17DELTA-PROPADIENYL-ESTRA-4,9(10)-DIENE-17BETA-O1-3-ONE OR THE 17BETA-ACETOXY DERIVATIVE THEREOF

机译:制备17delta-丙二烯基-estra-4,9(10)-diene-17BETA-O1-3-one或17beta-乙酰化衍生物的方法

摘要

1297964 17-Propadienyl-steroids SANDOZ Ltd 14 Nov 1969 [25 Nov 1968] 31038/72 Divided out of 1297962 Heading C2U The invention comprises 17-propadienyl- 17# - hydroxyestr - 4 - en - 3 - one (Ia) and 3#- acetoxy - 17 - propadienylestr - 4 - en - 17# - ol (Ib) and their preparation by complex metal hydride reduction of corresponding compounds having in the 17-position the group wherein R, RSP1/SP and RSP11/SP are each C 1-3 alkyl, or R is C 1-3 alkyl and NRSP1/SPRSP11/SP is pyrrolidino or piperidino, and Y is Cl, Br, I, OSO 2 Me or O-tosyl. Any 3-oxo group in the starting material is optionally protected, e.g. as a 3-methoxy- #SP2,5(10)/SP-compound, in which case a deprotection. step must follow the metal hydride reduction. Compound Ib is alternatively prepared by acetylating the corresponding free 3#-ol. The preparation of starting materials is as described in Specification 1,297,962. The inventive compounds are said to possess progestational activity, and may be made up with carriers into pharmaceutical compositions for oral and parenteral administration. Reference has been directed by the Comptroller to Specification 1,222,886.
机译:1297964 17-丙二烯基-甾族化合物SANDOZ Ltd 1969年11月14日[1968年11月25日] 31038/72从1297962税号C2U中分离本发明包含17-丙二烯基-17#-羟基雌二醇-4-en-3-一(Ia)和3# -乙酰氧基-17-丙二烯基雌二醇-4-en-17#-ol(Ib)及其通过复合金属氢化物还原制备在17位具有R,R 1 和R 11 分别为C 1-3烷基,或R为C 1-3烷基且NR 1 R 11 为吡咯烷基或哌啶子基, Y是Cl,Br,I,OSO 2 Me或O-甲苯磺酰基。起始材料中的任何3-氧代基团可任选地被保护,例如被保护。作为3-甲氧基-# 2,5(10)-化合物,在这种情况下为脱保护基。步骤必须跟随金属氢化物的还原。或者,通过乙酰化相应的游离3#-ol来制备化合物Ib。起始原料的制备如说明书1,297,962中所述。据说本发明的化合物具有孕激素活性,并且可以与载体一起制成药物组合物,用于口服和肠胃外给药。主计长已对规范1,222,886进行了引用。

著录项

  • 公开/公告号YU34534B

    专利类型

  • 公开/公告日1979-09-10

    原文格式PDF

  • 申请/专利权人 SANDOZ AG;

    申请/专利号YU19690002911

  • 申请日1969-11-20

  • 分类号C07J1/00;A61K31/56;

  • 国家 YU

  • 入库时间 2022-08-22 20:31:50

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