Process for the preparation of aprepitant
    4.
    发明授权
    Process for the preparation of aprepitant 有权
    制备阿司匹林的方法

    公开(公告)号:US08080656B2

    公开(公告)日:2011-12-20

    申请号:US12089297

    申请日:2006-10-05

    IPC分类号: C07D413/02 C07D295/00

    CPC分类号: C07D265/32 C07D413/06

    摘要: 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.

    摘要翻译: 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。

    PROCESS FOR THE PREPARATION OF APREPITANT
    6.
    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分类号: C07D265/32 C07D413/06

    摘要: 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.

    摘要翻译: 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。

    Stable lamotrigine pharmaceutical compositions and processes for their preparation
    8.
    发明申请
    Stable lamotrigine pharmaceutical compositions and processes for their preparation 审中-公开
    稳定的拉莫三嗪药物组合物及其制备方法

    公开(公告)号:US20070129549A1

    公开(公告)日:2007-06-07

    申请号:US10550173

    申请日:2004-03-22

    IPC分类号: C07D211/06

    摘要: The invention relates to processes for the preparation of piperidylmethyl-indanones, and to the use of these compounds as intermediates for the preparation of benzyl-piperidylmethyl-indanones which are active compounds for the treatment of CNS disorders. The invention also relates to a process for the preparation of donepezil or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions that include the donepezil or a pharmaceutically acceptable salt thereof.

    摘要翻译: 本发明涉及制备哌啶甲基 - 茚满酮的方法,以及这些化合物作为制备作为用于治疗CNS障碍的活性化合物的苄基 - 哌啶基甲基 - 茚满酮的中间体的用途。 本发明还涉及制备多奈哌齐或其药学上可接受的盐的方法,以及包含多奈哌齐或其药学上可接受的盐的药物组合物。