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    • 3. 发明授权
    • Process for preparing voriconazole by using new intermediates
    • 使用新中间体制备伏立康唑的方法
    • US08575344B2
    • 2013-11-05
    • US13577055
    • 2011-02-01
    • Hyuk Chul KwonMan Dong RhoKyung Hoi Cha
    • Hyuk Chul KwonMan Dong RhoKyung Hoi Cha
    • C07D403/06
    • C07D403/04C07D239/34C07D403/08
    • Provided is a process for preparing Voriconazole represented by Chemical Formula 1. More particularly, the process for preparing Voriconazole of Chemical Formula 1 includes: carrying out the Reformatsky-type coupling reaction between a ketone derivative of Chemical Formula 4 and a pyrimidine derivative of Chemical Formula 5 to obtain a compound of Chemical Formula 3; reacting the substituents halo and oxysulfonyl with a hydrogen donor to obtain racemic Voriconazole of Chemical Formula 2; and carrying out optical isolation of the racemic Voriconazole by adding an adequate optically active acid thereto to obtain Voriconazole having high optical purity with high cost-efficiency and high yield.
    • 提供一种用化学式1表示的伏立康唑的制备方法。更具体地说,制备化学式1的伏立康唑的方法包括:进行化学式4的酮衍生物与化学式的嘧啶衍生物之间的Reformatsky型偶联反应 得到化学式3的化合物; 使取代基卤代和氧基磺酰基与氢供体反应,得到化学式2的外消旋伏立康唑; 并通过向其中加入足够的光学活性酸进行外消旋的伏立康唑的光学分离,得到具有高成本效率和高产率的高光学纯度的伏立康唑。