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    A PROCESS FOR ETRA VIRINE INTERMEDIATE AND POLYMORPHS OF ETRAVIRINE
    6.
    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

    申请人： HETERO RESEARCH FOUNDATION

    发明人： PARTHASARADHI REDDY BANDI ,  RATHNAKAR REDDY KURA ,  MURALIDHARA REDDY DASARI ,  RAJI REDDY RAPOLU ,  VAMSI KRISHNA BANDI ,  VENKAT NARSIMHA REDDY ADULLA

    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。