PROCESS FOR THE PREPARATION OF APREPITANT
    51.
    发明申请
    PROCESS FOR THE PREPARATION OF APREPITANT 有权
    制定APRIPT的过程

    公开(公告)号:US20100004242A1

    公开(公告)日:2010-01-07

    申请号:US12089297

    申请日:2006-10-05

    CPC classification number: C07D265/32 C07D413/06

    Abstract: The present invention relates to a highly pure (2R,3S)-4-benzyl-3-(4-fluorophenyl)morpholin-2-yl 3,5-bis(trifluoromethyl)benzoate of Formula II, and a process for its preparation. The present invention further provides a process for preparation of Aprepitant of Formula I or pharmaceutically acceptable salt thereof, using the highly pure compound of Formula II. The present invention also provides a process for preparation of Aprepitant of Formula I or pharmaceutically acceptable salt thereof which comprises of cyclising the compound of Formula VII at elevated temperature, in the absence of solvent.

    Abstract translation: 本发明涉及式II的高纯度(2R,3S)-4-苄基-3-(4-氟苯基)吗啉-2-基3,5-双(三氟甲基)苯甲酸酯及其制备方法。 本发明还提供使用高度纯的式II化合物制备式I的阿维地丁或其药学上可接受的盐的方法。 本发明还提供了制备式I的阿维地敏剂或其药学上可接受的盐的方法,其包括在不存在溶剂的情况下在高温下使式VII的化合物环化。

    Rabeprazole calcium
    55.
    发明申请
    Rabeprazole calcium 审中-公开
    雷贝拉星钙

    公开(公告)号:US20060122233A1

    公开(公告)日:2006-06-08

    申请号:US10539681

    申请日:2003-12-16

    CPC classification number: C07D401/12

    Abstract: The present invention relates to calcium salts of rabeprazole and processes for preparing rabeprazole calcium. The invention also relates to pharmaceutical compositions that include the rabeprazole calcium and use of said compositions for the treatment or prevention of gastrointestinal ulcers

    Abstract translation: 本发明涉及雷贝拉唑的钙盐和雷贝拉唑钙的制备方法。 本发明还涉及包含雷贝拉唑钙的药物组合物和所述组合物用于治疗或预防胃肠溃疡的药物组合物

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