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    • 1. 发明专利
    • Production method of clopidogrel
    • 石蜡生产方法
    • JP2009029805A
    • 2009-02-12
    • JP2008179540
    • 2008-07-09
    • Cadila Healthcare Ltdカディラ ヘルスケア リミティド
    • PANDEY BIPINLOHRAY VIDYA BHUSHANLOHRAY BRAJ BHUSHAN
    • C07D495/04C07B57/00
    • C07D495/04
    • PROBLEM TO BE SOLVED: To provide a novel production method of thieno[3,2-c]pyridine derivative and its salt. SOLUTION: The production method comprises the following steps: (i) a compound of formula (V) or its salt is reacted with a cyanide of formula (VII) and a compound of formula (VI) is added, thus producing a racemic compound of formula (IV); (ii) the compound of formula (IV) in a (±) form or in an optically active (+) or (-) form is reacted with an acidic or basic reactant to obtain a compound of formula (II) or a salt holding its shape; (iii) the compound of formula (II) in a (±) form or in an optically active (+) or (-) form is reacted with an acidic reactant in the presence of methanol to obtain a compound of formula (I) or a salt holding its shape; (iv) and finally the (±) compound of formula (I) or its salt is divided into an optical isomer. COPYRIGHT: (C)2009,JPO&INPIT
    • 待解决的问题:提供噻吩并[3,2-c]吡啶衍生物及其盐的新型制备方法。 解决方案:制备方法包括以下步骤:(i)将式(Ⅴ)化合物或其盐与式(Ⅶ)的氰化物反应,加入式(Ⅵ)化合物,从而产生 式(IV)的外消旋化合物; (ii)以(±)形式或光学活性(+)或( - )形式的式(IV)化合物与酸性或碱性反应物反应,得到式(II)化合物或其盐 其形状; (iii)以(±)形式或光学活性(+)或( - )形式的式(II)化合物与甲酸存在下的酸性反应物反应,得到式(I)或 保持其形状的盐; (iv),最后将式(I)的(±)化合物或其盐分成旋光异构体。 版权所有(C)2009,JPO&INPIT