Process for the preparation of ziprasidone
    84.
    发明授权
    Process for the preparation of ziprasidone 失效
    齐拉西酮制备方法

    公开(公告)号:US08178674B2

    公开(公告)日:2012-05-15

    申请号:US13100833

    申请日:2011-05-04

    CPC classification number: C07D417/12

    Abstract: The invention relates to processes for the preparation of substantially pure ziprasidone. The invention also relates to the preparation of acid addition salts of ziprasidone. More particularly, it relates to the preparation of substantially pure hydrochloride salt of ziprasidone. The invention also relates to pharmaceutical compositions that include the substantially pure ziprasidone or ziprasidone hydrochloride and use of said compositions for treating schizophrenia.

    Abstract translation: 本发明涉及制备基本上纯的齐拉西酮的方法。 本发明还涉及齐拉西酮的酸加成盐的制备。 更具体地说,本发明涉及齐拉西酮基本上纯的盐酸盐的制备。 本发明还涉及药物组合物,其包括基本上纯的齐拉西酮或齐拉昔酮盐酸盐以及所述组合物用于治疗精神分裂症的用途。

    Process for the preparation of aprepitant
    86.
    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

    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。

    Processes for the preparation of substituted sulfoxides
    87.
    发明授权
    Processes for the preparation of substituted sulfoxides 有权
    制备取代亚砜的方法

    公开(公告)号:US07915422B2

    公开(公告)日:2011-03-29

    申请号:US11576867

    申请日:2005-10-04

    CPC classification number: C07D401/12

    Abstract: The present invention relates to a process for enantioselective synthesis of substituted pyridinylmethyl sulfinyl-benzimidazole of compound of Formula (I). The process includes enantioselective catalytic oxidation of a substituted pyridinylmethyl prochiral sulfide derivative of compound of Formula (II) with an oxidizing agent in the presence of a chiral transition metal complex and a base in the absence of an organic solvent.

    Abstract translation: 本发明涉及式(I)化合物的取代的吡啶基甲基亚磺酰基 - 苯并咪唑的对映选择性合成方法。 该方法包括式(II)化合物的取代的吡啶基甲基前手性硫化物衍生物在手性过渡金属络合物和碱的存在下,在不存在有机溶剂的情况下与氧化剂的对映选择性催化氧化。

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