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12 条记录 (耗时 0.063 秒)

    Process for the preparation of sorafenib and salts thereof
    6.
    发明申请
    Process for the preparation of sorafenib and salts thereof 审中-公开
    索拉非尼及其盐的制备方法

    公开(公告)号：US20090253913A1

    公开(公告)日：2009-10-08

    申请号：US12381000

    申请日：2009-03-05

    申请人： Pierluigi Rossetto ,  Peter Lindsay MacDonald ,  Augusto Canavesi

    发明人： Pierluigi Rossetto ,  Peter Lindsay MacDonald ,  Augusto Canavesi

    IPC分类号： C07D213/78 ,  C07D233/14

    CPC分类号： C07D233/61 ,  C07D213/81

    摘要： Methods for the synthesis of the N-carbamoyl imidazole (I) and its 1:1 adduct with imidazole are provided. Methods for the preparation of these crystalline intermediates in a high state of purity are also provided. These intermediates react cleanly under mild conditions to produce sorafenib in high yield and purity, without generating difficult-to-remove impurities.

    摘要翻译： 提供了合成N-氨基甲酰基咪唑（I）及其与咪唑的1:1加合物的方法。 还提供了制备高纯度的这些结晶中间体的方法。 这些中间体在温和条件下干净地反应以高产率和纯度产生索拉非尼，而不产生难以除去的杂质。

    Process for the preparation of letrozole
    10.
    发明授权
    Process for the preparation of letrozole 失效
    来曲唑的制备方法

    公开(公告)号：US07705159B2

    公开(公告)日：2010-04-27

    申请号：US11482228

    申请日：2006-07-06

    申请人： Peter Lindsay MacDonald ,  Ettore Bigatti ,  Pierluigi Rossetto ,  Zvi Harel

    发明人： Peter Lindsay MacDonald ,  Ettore Bigatti ,  Pierluigi Rossetto ,  Zvi Harel

    IPC分类号： C07D249/08

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： The invention provides a high-yield process for the preparation of letrozole having a high purity, without the need for removal of the 4-[1-(1,3,4-triazolyl)methyl]benzonitrile impurity at the intermediate stage. The invention also provides a process for the synthesis of letrozole in which formation of the impurity 4-[1-(1,3,4-triazolyl)methyl]benzonitrile during the first stage is minimized. In the process, a 4-(halomethyl)benzonitrile is reacted with a salt of 1H-1,2,4-triazole, reducing the formation of the impurity. Preferably, the preparation is conducted as a one-pot process.

    摘要翻译： 本发明提供了用于制备具有高纯度的来曲唑的高产率方法，而不需要在中间阶段除去4- [1-（1,3,4-三唑基）甲基]苄腈杂质。 本发明还提供合成来曲唑的方法，其中第一阶段期间杂质4- [1-（1,3,4-三唑基）甲基]苄腈的形成最小化。 在此过程中，使4-（卤代甲基）苄腈与1H-1,2,4-三唑的盐反应，减少杂质的形成。 优选地，制备是作为一锅法进行的。