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    Process for preparing temozolomide
    1.
    发明授权
    Process for preparing temozolomide 失效
    替莫唑胺制备方法

    公开(公告)号：US07612202B2

    公开(公告)日：2009-11-03

    申请号：US11354899

    申请日：2006-02-16

    申请人： Olga Etlin ,  Mohammed Alnabari ,  Yana Sery ,  Edna Danon ,  Oded Arad ,  Joseph Kaspi

    发明人： Olga Etlin ,  Mohammed Alnabari ,  Yana Sery ,  Edna Danon ,  Oded Arad ,  Joseph Kaspi

    IPC分类号： C07D487/04 ,  A61K31/395 ,  A61P35/00

    CPC分类号： C07D487/04 ,  B01J39/07 ,  B01J41/07 ,  B01J49/00 ,  B01J49/06 ,  B01J49/07

    摘要： The present invention provides a process for preparing highly pure Temozolomide base which includes recovery from the purification mother liquors by using an anionic exchange resin. By treating Temozolomide hydrochloride with a mixture of an organic acid, a water miscible organic solvent, and water, Temozolomide free base is obtained in an acidic medium. Due to the high sensitivity of Temozolomide to basic pH values the recovery-including process is especially advantageous because it enables obtaining high yields of highly pure Temozolomide base in acidic conditions.The process for producing Temozolomide base includes hydrolysis of the starting material 8-cyano-3-methyl-[3H]-imidazo[5,1-d]-tetrazin-4-one in acidic medium to obtain highly pure Temozolomide hydrochloride in high yield.

    摘要翻译： 本发明提供了制备高纯度替莫唑胺碱的方法，其包括通过使用阴离子交换树脂从纯化母液中回收。 通过用有机酸，水混溶性有机溶剂和水的混合物处理盐酸替莫唑胺，在酸性介质中获得替莫唑胺游离碱。 由于替莫唑胺对碱性pH值的高敏感性，回收包含的方法是特别有利的，因为它能够在酸性条件下获得高产量的高纯度替莫唑胺碱。 制备替莫唑胺碱的方法包括在酸性介质中水解原料8-氰基-3-甲基 - [3 H] - 咪唑并[5,1-d] - 四嗪-4-酮，以高产率得到高纯度的替莫唑胺盐酸盐 。