发明授权
US3929769A Process for the manufacture of steroid epoxides 失效
类固醇环氧化物的制造方法

  • 专利标题: Process for the manufacture of steroid epoxides
  • 专利标题(中): 类固醇环氧化物的制造方法
  • 申请号: US45126174
    申请日: 1974-03-14
  • 公开(公告)号: US3929769A
    公开(公告)日: 1975-12-30
  • 发明人: KAUFMANN HEINZWETTSTEIN ALBERT
  • 申请人: CIBA GEIGY CORP
  • 专利权人: Ciba Geigy Corp
  • 当前专利权人: Ciba Geigy Corp
  • 优先权: US45126174 1974-03-14; CH747972 1972-05-19; US36023073 1973-05-14
  • 主分类号: C07J17/00
  • IPC分类号: C07J17/00
Process for the manufacture of steroid epoxides
摘要:
wherein X1 is chlorine or fluorine, X2 is chlorine, fluorine or trifluoromethyl and R and R'' are alkyl groups or together with the nitrogen atom form a heterocyclic radical. There are preferably used compounds in which R and R'' are lower alkyl groups, such as for instance N- (2-chloro-1,1,2-trifluoroethyl)diethylamine, and the reaction is performed in an inert solvent e.g. ethylene chloride, at room temperature or elevated temperature, if desired, in the presence of another organic nitrogen base. The compounds of the process are intermediates for the preparation of therapeutically useful 6-fluoro-steroids, such as 6-fluoro-corticoids. In particular, the epoxides can be further reacted with the same fluorinated amine used in their preparation to give the 6 Beta ,5 Alpha -fluorohydrins.

The invention is directed to a process for the manufacture of 5 Alpha ,6 Alpha -oxido-steroids starting from corresponding 5 Alpha ,6 Beta -dihydroxy steroids. The starting steroids are treated with a fluorinated amine of the formula
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