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    Novel Process
    13.
    发明申请
    Novel Process 审中-公开
    小说流程

    公开(公告)号：US20080182848A1

    公开(公告)日：2008-07-31

    申请号：US11961673

    申请日：2007-12-20

    Applicant: Debashish Datta ,  Ajaysingh Rawat ,  Shardard N. Duche ,  E.K.S. Vijayakumar

    Inventor： Debashish Datta ,  Ajaysingh Rawat ,  Shardard N. Duche ,  E.K.S. Vijayakumar

    IPC: A61K31/4985 ,  C07D487/04 ,  A61P25/22 ,  A61P25/24 ,  A61P25/00

    CPC classification number: C07D487/04

    Abstract: The present invention relates to a process for optically resolving eszopiclone, comprising chiral chromatography. Preferably the process comprises a multi-column continuous process or a simulated moving bed process. Preferably the stationary phase used in the chiral chromatography process comprises an amylose or cellulose derivative of tris(3,5-dimethylphenyl carbamate), or an amylose derivative of tris-α-methylbenzylcarbamate. The process of the present invention has the advantage that it is high yielding and can be carried out on an industrial scale.The present invention also provides eszopiclone, or a pharmaceutically acceptable salt thereof, obtained by the chiral chromatography process. The eszopiclone or salt thereof is suitable for use as a medicament, for example, for the treatment of anxiety or insomnia.

    Abstract translation: 本发明涉及一种光学拆分依佐氟龙的方法，包括手性色谱法。 优选地，该方法包括多塔连续方法或模拟移动床方法。 优选地，用于手性色谱法的固定相包括三（3,5-二甲基苯基氨基甲酸酯）的直链淀粉或纤维素衍生物，或三-α-甲基苄基氨基甲酸酯的直链淀粉衍生物。 本发明的方法具有高产量并且可以在工业规模上进行的优点。 本发明还提供了通过手性色谱法获得的依佐溴隆或其药学上可接受的盐。 右佐佐酮或其盐适合用作药物，例如用于治疗焦虑或失眠。

    Process for preparation of perindopril and salts thereof
    15.
    发明申请
    Process for preparation of perindopril and salts thereof 有权
    培哚普利及其盐的制备方法

    公开(公告)号：US20060276659A1

    公开(公告)日：2006-12-07

    申请号：US10547243

    申请日：2003-02-28

    Applicant: Debashish Datta ,  Girij Singh ,  Himanshu Godbole ,  Rajinder Siyan

    Inventor： Debashish Datta ,  Girij Singh ,  Himanshu Godbole ,  Rajinder Siyan

    IPC: C07D209/42

    CPC classification number: C07D209/42 ,  C07C227/32 ,  C07C227/34 ,  C07C229/12

    Abstract: A process for preparation of perindopril of formula (II) and salts thereof which is simple, safe convenient and cost-effective. The process involves reaction of compound of formula (I), wherein X is chlorine or bromine with compound of formula (VII) wherein A signifies that the six-membered ring of the bicyclic system is either saturated or unsaturated to give compound of formula (VIII), wherein A is as defined above, followed by catalytic hydrogenation of the compound of formula (VIII) thus obtained to give the perindopril of formula (II). The above process for the manufacture of perindopril would specifically avoid the use of harmful chemicals like phosgene or costly coupling agents like dicyclohexylcarbodiimide and 1-hydroxybenxotriazole usually used for such manufacture. The process would also not require any intervention of a catalyst and does not require any alkaline or acidic reaction conditions. Importantly, the process provides for manufacture of perindopril with high stereoselectively giving perindopril (II) having (S)-configuration in all the five chiral centres of the molecule, conforming to pharmacoepeial specifications. The invention also relates to a method for preparation of the compound of formula (I) and also to a method for preparation of N-[(S)-1-carbethoxybutyl]-(S)-alanine of formula (III) used in the process.

    Abstract translation: 制备式（II）的培哚普利及其盐的方法，其简单，安全的方便和成本有效。 该方法包括式（I）化合物，其中X是氯或溴与式（Ⅶ）化合物反应，其中A表示双环系统的六元环是饱和或不饱和的，得到式（Ⅷ）化合物 ），其中A如上所定义，然后将由此获得的式（VIII）化合物进行催化氢化，得到式（II）的培哚普利。 上述制造培哚普利的方法将特别避免使用通常用于制造的有害化学物质如光气或昂贵的偶联剂如二环己基碳二亚胺和1-羟基苯并三唑。 该方法也不需要任何催化剂的干预，并且不需要任何碱性或酸性反应条件。 重要的是，该方法提供了高度立体选择性地给予符合药代动力学规范的在分子的所有五个手性中心具有（S） - 构型的培哚普利（II）的培哚普利的培哚普利。 本发明还涉及制备式（I）化合物的方法，还涉及制备式（III）化合物的N - [（S）-1-甲氧基丁基] - （S） - 丙氨酸的方法， 处理。

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