Process for the preparation of sorafenib and salts thereof
    8.
    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

    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 pregnanes
    9.
    发明申请
    Process for the preparation of pregnanes 审中-公开
    孕妇的制备方法

    公开(公告)号:US20060252926A1

    公开(公告)日:2006-11-09

    申请号:US10537916

    申请日:2003-12-02

    IPC分类号: C07J71/00

    CPC分类号: C07J71/0015

    摘要: An improved stereoselective process for the preparation of 6α-fluoropregnane derivatives of formula (I), comprising the reaction of 3-benzoyloxy Δ3,5-pregnane derivatives of formula (II), with an electrophilic fluorination agent in a substantially water-free reaction mixture and in the presence of a salt of a strong acid with a nitrogenous base.

    摘要翻译: 一种用于制备式(I)的6α-氟代孕烷衍生物的改进的立体选择性方法,包括式(II)的3-苯甲酰氧基Delta3,5-孕烷衍生物与亲电氟化剂在基本上无水的反应混合物 并存在强酸与含氮碱的盐的存在下。