AN IN-SITU PROCESS FOR THE PREPARATION OF HIGHLY PURE MONTELUKAST SODIUM
    3.
    发明申请
    AN IN-SITU PROCESS FOR THE PREPARATION OF HIGHLY PURE MONTELUKAST SODIUM 审中-公开
    用于制备高纯度蒙特梭菌钠的现场方法

    公开(公告)号:WO2014118796A1

    公开(公告)日:2014-08-07

    申请号:PCT/IN2013/000312

    申请日:2013-05-13

    CPC classification number: C07D215/18

    Abstract: The present invention disclosed herein is a cost effective, in-situ process for the preparation of montelukast or its pharmaceutically acceptable salts of formula (1) by reacting optically pure (S)-1-{3-[2-(7-chloroquinolin-2-yl)ethylene]-phenyl}-3-[2-(1-hydroxy-1-methyl ethyl) phenyl]-propan-I-ol with methane sulfonyl chloride to afford mesylate derivative of formula (2) substantially free of impurities; followed by insitu condensing the same with disodium salt of mercapto-cyclopropyl acetic acid of formula (3) to afford montelukast free acid in good yield and purity, then converting the montelukast free acid into its substituted amine salt of formula (4). Further the montelukast substituted amine is converted into its pharmaceutically acceptable salt.

    Abstract translation: 本文公开的本发明是通过使光学纯的(S)-1- {3- [2-(7-氯喹啉-2-基) 吡啶-2-基)乙烯] - 苯基} -3- [2-(1-羟基-1-甲基乙基)苯基] - 丙-1-醇与甲磺酰氯反应,得到基本上不含杂质的式(2)的甲磺酸酯衍生物 ; 然后将其与式(3)的巯基 - 环丙基乙酸的二钠盐相同地进行缩合,得到良好的产率和纯度的孟鲁司特游离酸,然后将孟鲁司特游离酸转化为式(4)的取代的胺盐。 此外,孟鲁司特胺取代的胺被转化成其药学上可接受的盐。

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