PROCESS FOR PREPARATION OF SOLID MONTELUKAST
    5.
    发明申请
    PROCESS FOR PREPARATION OF SOLID MONTELUKAST 审中-公开
    固体蒙特卡松的制备方法

    公开(公告)号:US20100063291A1

    公开(公告)日:2010-03-11

    申请号:US12619736

    申请日:2009-11-17

    IPC分类号: C07D215/14

    CPC分类号: C07D215/18

    摘要: A process for preparation of montelukast or a salt thereof is provided, the process including reacting a late intermediate compound which is 2-[1-[1-R-3-[2-(7 chloro quinolin-2-yl)vinyl [phenyl]-3-[2-methoxy carbonyl phenyl]propyl sulfonyl methyl]cyclo propyl]acetic acid or a salt thereof with methyl magnesium chloride or methyl magnesium bromide in an organic solvent. In one embodiment, the process includes reacting an earlier intermediate compound which is methyl 2-(3-R-(3-(2-(7-chloro 2-quinolinyl)-ethenyl)-3 hydroxy propyl)benzoate with methane sulfonyl chloride or toluene sulfonyl chloride to obtain a mesylated or tosylated derivative of the earlier intermediate compound; followed by a reaction of the mesylated or tosylated derivative with 1-mercapto methyl cyclopropane acetic acid in a polar solvent in a presence of a base to obtain the late intermediate compound.

    摘要翻译: 提供了一种制备孟鲁司特或其盐的方法,该方法包括使2- [1- [1- [3- [2-(7-氯喹啉-2-基)乙烯基] [苯基 ] -3- [2-甲氧基羰基苯基]丙基磺酰基甲基]环丙基]乙酸或其盐与甲基氯化镁或甲基溴化镁在有机溶剂中反应。 在一个实施方案中,该方法包括使2-(3-R-(3-(2-(7-氯-2-喹啉基) - 乙烯基)-3-羟基丙基)苯甲酸甲酯与甲磺酰氯反应的较早中间体化合物或 甲磺酰氯,得到较早期中间体化合物的甲磺酰化或甲磺酰化衍生物;随后在极性溶剂中,在碱的存在下,使甲磺酰化或甲硅烷基化衍生物与1-巯基甲基环丙烷乙酸反应,得到后期中间体化合物 。