发明公开
EP0264880A1 Fluorine derivatives of vitamin D3 and process for producing the same
失效
的维生素D3和其制备方法的氟化的衍生物。
- 专利标题： Fluorine derivatives of vitamin D3 and process for producing the same
- 专利标题（中）： 的维生素D3和其制备方法的氟化的衍生物。
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申请号： EP87115258.3申请日： 1987-10-19
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公开(公告)号： EP0264880A1公开(公告)日： 1988-04-27
- 发明人: Hamma, Noritaka , Nishizawa, Toshio , Saito, Yoshikazu , Katsumata, Takashi
- 申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED
- 申请人地址： 2-8, Doshomachi 2-chome, Chuo-ku Osaka-shi Osaka-fu JP
- 专利权人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED
- 当前专利权人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED
- 当前专利权人地址： 2-8, Doshomachi 2-chome, Chuo-ku Osaka-shi Osaka-fu JP
- 代理机构： VOSSIUS & PARTNER
- 优先权： JP249095/86 19861020
- 主分类号： C07C401/00
- IPC分类号： C07C401/00 ; A61K31/59
摘要：
There are disclosed novel derivatives of 26,26,26,27,27,27-hexafluorovitamin D₃ having a fluorine atom at the 23- and/or 24-position which have an excellent pharmacological activity and a process for production thereof. The novel compounds are represented by the general formula (1).
wherein R₁ʹ denotes a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R₂ denotes a hydrogen atom or a protecting group for a hydroxyl group, R₃ denotes a hydrogen atom, a fluorine atom, a hydroxyl group or a protected hydroxyl group and R₄ and R₄ʹ each denotes a hydrogen atom, or one of them denotes a hydrogen atom and the other denotes a fluorine atom, hydroxyl group or a protected hydroxyl group or R₄ and R₄ are combined to denote an oxo group, with a proviso that at least one of R₃, R₄ and R₄ʹ denotes a fluorine atom. The process for production thereof comprises subjecting a compound represented by the general formula (3)
wherein R₁ʹ, R₂, R₃, R₄ and R₄ʹ are the same as defined above, to thermal isomerization and optionally further to a deprotection reaction.
wherein R₁ʹ denotes a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R₂ denotes a hydrogen atom or a protecting group for a hydroxyl group, R₃ denotes a hydrogen atom, a fluorine atom, a hydroxyl group or a protected hydroxyl group and R₄ and R₄ʹ each denotes a hydrogen atom, or one of them denotes a hydrogen atom and the other denotes a fluorine atom, hydroxyl group or a protected hydroxyl group or R₄ and R₄ are combined to denote an oxo group, with a proviso that at least one of R₃, R₄ and R₄ʹ denotes a fluorine atom. The process for production thereof comprises subjecting a compound represented by the general formula (3)
wherein R₁ʹ, R₂, R₃, R₄ and R₄ʹ are the same as defined above, to thermal isomerization and optionally further to a deprotection reaction.
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