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    Process of lactonization in the preparation of statins
    8.
    发明授权
    Process of lactonization in the preparation of statins 失效
    内酯化制备他汀类药物的过程

    公开(公告)号：US5917058A

    公开(公告)日：1999-06-29

    申请号：US64285

    申请日：1998-04-22

    申请人： Yatendra Kumar ,  Rajesh Kumar Thaper ,  S. M. Dileep Kumar ,  Jag Mohan Khanna

    发明人： Yatendra Kumar ,  Rajesh Kumar Thaper ,  S. M. Dileep Kumar ,  Jag Mohan Khanna

    IPC分类号： C07D309/30

    CPC分类号： C07D309/30

    摘要： An improved process of lactonization in the preparation of statins (e.g., the HMG--CoA reductase inhibitors lovastatin and simvastatin) employs very mild reaction conditions. The improved process comprises treating the open ring hydroxy acid form of the statins with an excess of acetic acid and in the absence of a strong acid catalyst under mild heating conditions (e.g., ambient to 55.degree. C.), and adding an anti-solvent to the reaction mixture, thereby causing the statins in lactone form to crystalize from the reaction mixture. The acetic acid serves as both a solvent and a catalyst for the lactonization reaction.

    摘要翻译： 在制备他汀类药物（例如，HMG-CoA还原酶抑制剂洛伐他汀和辛伐他汀）中改进的内酯化方法采用非常温和的反应条件。 改进的方法包括用温和的加热条件（例如，环境温度至55℃）用过量的乙酸处理开环羟基酸形式的他汀类和不存在强酸催化剂的情况下，加入抗溶剂 反应混合物，从而使内酯形式的他汀类从反应混合物中结晶。 乙酸既用作内酯化反应的溶剂和催化剂。