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    Fluorine derivatives of vitamin D3 and process for producing the same
    1.
    发明公开
    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。

    公开(公告)号：EP0264880A1

    公开(公告)日：1988-04-27

    申请号：EP87115258.3

    申请日：1987-10-19

    申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED

    发明人： Hamma, Noritaka ,  Nishizawa, Toshio ,  Saito, Yoshikazu ,  Katsumata, Takashi

    IPC分类号： C07C401/00 ,  A61K31/59

    CPC分类号： C07C401/00 ,  C07J9/00 ,  C07J71/001 ,  Y02P20/55

    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.

    摘要翻译： 存在具有在23-和/或24位上其具有优异的药理学活性和其制备方法是氟原子26,26,26,27,27,27-hexafluorovitamin D3的游离缺失盘新的衍生物。 的新化合物是由通式（1）表示。 worin R1“表示氢原子，羟基或保护的羟基，R 2表示氢原子或羟基的保护基团，R3表示氢原子，氟原子，羟基或被保护的 羟基和R 4和R 4“各自表示氢原子，或它们中的一个表示氢原子且另一个表示氟原子，羟基或保护的羟基基团或R 4和R 4结合，以表示于氧代基团，具有 条件没有R3，R4和R4“中的至少一个表示氟原子。 生产过程中其包括使由通式（3） worin R1，R2，R3，R4和R4“表示的化合物是相同的如上述所定义，热异构化并任选地进一步脱保护反应。