Process for the preparation of pregnanes
    4.
    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。

    Process for the preparation of letrozole
    8.
    发明申请
    Process for the preparation of letrozole 失效
    来曲唑的制备方法

    公开(公告)号:US20070066831A1

    公开(公告)日:2007-03-22

    申请号:US11482228

    申请日:2006-07-06

    IPC分类号: 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。