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    Process of lactonization in the preparation of statins
    3.
    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。

    Key intermediates in the manufacture of simvastatin
    4.
    发明授权
    Key intermediates in the manufacture of simvastatin 失效
    辛伐他汀制造中的关键中间体

    公开(公告)号：US5763653A

    公开(公告)日：1998-06-09

    申请号：US816574

    申请日：1997-03-13

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

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

    IPC分类号： C07C231/00 ,  C07C235/30 ,  C07D309/30 ,  C07C67/02

    CPC分类号： C07C235/30 ,  C07D309/30 ,  C07C2101/02 ,  C07C2102/28

    摘要： A process for preparing simvastatin from lovastatin or mevinolinic acid in salt form comprises treating either starting material with cyclopropyl or butyl amine, the pyranone ring thereby being opened when lovastatin is the starting material, adding a methyl group to the 2-methylbutyrate side chain, and thereafter closing the open pyranone ring to produce simvastatin. The process is performed without protecting and deprotecting the two hydroxy groups of the open pyranone ring. In a preferred embodiment, the starting material is treated with cyclopropyl amine which produces simvastatin via the novel intermediate lovastatin cyclopropyl amide.

    摘要翻译： 以盐形式从洛伐他汀或甲维林酸制备辛伐他汀的方法包括用环丙基或丁胺处理起始原料，当洛伐他汀为原料时，吡喃酮环由此开放，向2-甲基丁酸酯侧链加入甲基， 然后关闭开放的吡喃酮环以产生辛伐他汀。 在不保护和去保护开放式吡喃酮环的两个羟基的情况下进行该方法。 在优选的实施方案中，用环丙胺处理起始物质，其通过新的中间体洛伐他汀环丙基酰胺产生辛伐他汀。

    Process of lactonization in the preparation of statins
    6.
    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：US5939564A

    公开(公告)日：1999-08-17

    申请号：US055572

    申请日：1998-04-06

    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： A novel process of lactonizaton in the preparation of statins (e.g., the HMG--CoA reductase inhibitors lovastatin and simvastatin) employs very mild reaction conditions. The improved process comprises dissolving the open ring hydroxy acid form of the statins in an organic solvent by heating at a temperature, which ranges from ambient to reflux of the solvent, under anhydrous conditions to produce a solution, treating the solution with a mild catalyst at a temperature from about ambient to 50.degree. C., and adding water to the solution to cause the statins in lactone form to crystalize from the reaction mixture. The mild catalyst used in the reaction is a salt of an organic base with an organic or inorganic acid, such as pyridine hydrobromide, pyridine hydrochloride, or pyridinium, p-toluene sulfonate. The organic solvent comprises a lower alkanol, a non-alcoholic polar solvent, or a mixture of the two.

    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）中的新方法使用非常温和的反应条件。 改进的方法包括通过在无水条件下从环境温度至溶剂回流的温度加热，将开环羟基酸形式的他汀类药物溶解在有机溶剂中，以产生溶液，用温和的催化剂处理溶液 温度为约环境温度至50℃，并向溶液中加入水，使得内酯形式的他汀类从反应混合物中结晶。 反应中使用的温和催化剂是有机碱与有机或无机酸的盐，例如吡啶氢溴酸盐，吡啶盐酸盐或吡啶鎓对甲苯磺酸盐。 有机溶剂包括低级链烷醇，非醇极性溶剂或两者的混合物。

    Process for manufacturing simvastatin from lovastatin or mevinolinic acid
    7.
    发明授权
    Process for manufacturing simvastatin from lovastatin or mevinolinic acid 失效
    从洛伐他汀或甲维林酸生产辛伐他汀的方法

    公开(公告)号：US5763646A

    公开(公告)日：1998-06-09

    申请号：US816573

    申请日：1997-03-13

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

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

    IPC分类号： C07D309/30 ,  C07C67/02

    CPC分类号： C07D309/30

    摘要： A process for preparing simvastatin from lovastatin or mevinolinic acid in salt form comprises treating either starting material with cyclopropyl or butyl amine, the pyranone ring thereby being opened when lovastatin is the starting material, adding a methyl group to the 2-methylbutyrate side chain, and thereafter closing the open pyranone ring to produce simvastatin. The process is performed without protecting and deprotecting the two hydroxy groups of the open pyranone ring. In a preferred embodiment, the starting material is treated with cyclopropyl amine which produces simvastatin via the novel intermediate lovastatin cyclopropyl amide.

    摘要翻译： 以盐形式从洛伐他汀或甲维林酸制备辛伐他汀的方法包括用环丙基或丁胺处理起始原料，当洛伐他汀为原料时，吡喃酮环由此开放，向2-甲基丁酸酯侧链加入甲基， 然后关闭开放的吡喃酮环以产生辛伐他汀。 在不保护和去保护开放式吡喃酮环的两个羟基的情况下进行该方法。 在优选的实施方案中，用环丙胺处理起始物质，其通过新的中间体洛伐他汀环丙基酰胺产生辛伐他汀。