A PROCESS FOR ETRA VIRINE INTERMEDIATE AND POLYMORPHS OF ETRAVIRINE
    4.
    发明公开
    A PROCESS FOR ETRA VIRINE INTERMEDIATE AND POLYMORPHS OF ETRAVIRINE 审中-公开
    VERFAHRENFÜRETRAVIRINZWISCHENPRODUKT UND POLYMORPHE VON ETRAVIRIN

    公开(公告)号:EP2584901A4

    公开(公告)日:2013-10-09

    申请号:EP10854026

    申请日:2010-06-28

    IPC分类号: A01N43/54 A61K31/505

    CPC分类号: C07D239/47 A61K31/505

    摘要: 4-[[6-chloro-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl-benzonitrile is a key intermediate for the preparation of etravirine. The present invention provides a process for preparation of 4-[[6-chloro-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethylbenzonitrile. The present invention also provides a novel process for the preparation of etravirine crystalline form I. The present invention further provides novel crystalline forms of etravirine, processes for their preparation and pharmaceutical compositions comprising them.

    摘要翻译: 4 - [[6-氯-2 - [(4-氰基苯基)氨基] -4-嘧啶基]氧基] -3,5-二甲基 - 苯甲腈是制备依曲韦林的关键中间体。 本发明提供了制备4 - [[6-氯-2 - [(4-氰基苯基)氨基] -4-嘧啶基]氧基] -3,5-二甲基苄腈的方法。 本发明还提供了制备依曲韦林结晶形式I的新方法。本发明进一步提供了依曲韦林的新结晶形式,它们的制备方法和包含它们的药物组合物。