Processing method of lactionization in the preparation of statins
    2.
    发明授权
    Processing method of lactionization in the preparation of statins 失效
    他汀类药物制剂的加工方法

    公开(公告)号:US06906204B2

    公开(公告)日:2005-06-14

    申请号:US10295300

    申请日:2002-11-14

    CPC分类号: C07D309/30

    摘要: The present invention relates to a processing method for preparing lovastatin and simvastatin which comprises the steps of (1) performing lactonization of mevinic acid and its homologous compounds in the presence of a mixed organic solvent without an acid catalyst through nitrogen sweep; and (2) making crystals. In the process of the present invention, lovastatin and simvastatin highly purified can be produced in a high yield and especially, heterodimers formed as a by-product can be reduced remarkably. Therefore, the processing method of the present invention can be convenient and economical.

    摘要翻译: 本发明涉及一种制备洛伐他汀和辛伐他汀的加工方法,该方法包括以下步骤:(1)通过氮气吹扫在无酸催化剂的混合有机溶剂的存在下进行乙酸及其同系化合物的内酯化; 和(2)制造晶体。 在本发明的方法中,可以高产率地制备高度纯化的洛伐他汀和辛伐他汀,特别是作为副产物形成的异二聚体可以显着降低。 因此,本发明的处理方法可以方便和经济。

    Process of lactonization in the preparation of statins
    4.
    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:US06649775B2

    公开(公告)日:2003-11-18

    申请号:US10200174

    申请日:2002-07-23

    IPC分类号: C07D30910

    CPC分类号: C07D309/30

    摘要: The present invention relates to a process for preparing lovastatin and simvastatin which comprises (1) performing step of a lactonization of mevinic acid and analog thereof compounds in the presence of a dehydrating agent and without an acid catalyst under nitrogen sweep; and then (2) making step of crystals at a high temperature. In the process of the present invention, lovastatin and simvastatin highly purified can be produced in a high yield and especially, heterodimers formed as a by-product can be reduced in an amount remarkably. Therefore, the process of the present invention is convenient and economical.

    摘要翻译: 本发明涉及一种制备洛伐他汀和辛伐他汀的方法,该方法包括:(1)在脱水剂存在下,在氮气吹扫下,不用酸催化剂进行乙酸及其类似物的内酯化步骤; 然后(2)在高温下进行晶体化步骤。 在本发明的方法中,可以高产率地制备高度纯化的洛伐他汀和辛伐他汀,特别是可以显着降低作为副产物形成的异二聚体。 因此,本发明的方法是方便和经济的。