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    Process for Producing Pure Form of 2-Methyl-4-(4-Methyl-1-Piperazinyl)-10H-Thieno[2,3-b] [1,5]Benzodiazepine
    46.
    发明申请
    Process for Producing Pure Form of 2-Methyl-4-(4-Methyl-1-Piperazinyl)-10H-Thieno[2,3-b] [1,5]Benzodiazepine 失效
    制备2-甲基-4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂

    公开(公告)号：US20090005556A1

    公开(公告)日：2009-01-01

    申请号：US11632362

    申请日：2004-07-14

    Applicant: Jwalant Ashesh Shastri ,  Akshat Bhatnagar ,  Rajesh Kumar Thaper ,  Sushil Kumar Dubey

    Inventor： Jwalant Ashesh Shastri ,  Akshat Bhatnagar ,  Rajesh Kumar Thaper ,  Sushil Kumar Dubey

    IPC: C07D487/04

    CPC classification number: C07D495/04 ,  C07D243/10 ,  C07D333/38

    Abstract: Disclosed is a process for producing pure form of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine. The process comprises of reacting 2-(2-aminoanilino)-5-methylthiophene-3-carbonitrile with N-methyl piperazine in conjunction with N-methylpiperazine acid salt, to produce 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine. Also disclosed is a process for obtaining the Polymorphic Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine by crystallizing the crude 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine in a mixture of solvents.

    Abstract translation: 公开了一种生产纯形式的2-甲基-4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂的方法。 该方法包括使2-（2-氨基苯胺基）-5-甲基噻吩-3-腈与N-甲基哌嗪与N-甲基哌嗪酸盐一起反应，得到2-甲基-4-（4-甲基-1-哌嗪基 ）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂。 还公开了2-甲基-4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂的多晶型I的方法， 甲基-4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂在溶剂混合物中。

    Process of lactonization in the preparation of statins
    47.
    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

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

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

    IPC: C07D309/30

    CPC classification number: C07D309/30

    Abstract: 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.

    Abstract translation: 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
    48.
    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

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

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

    IPC: C07D309/30 ,  C07C67/02

    CPC classification number: C07D309/30

    Abstract: 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.

    Abstract translation: 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。

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