Process for preparing montelukast and precursors thereof
    2.
    发明申请
    Process for preparing montelukast and precursors thereof 审中-公开
    孟鲁司特及其前体的制备方法

    公开(公告)号:US20060223999A1

    公开(公告)日:2006-10-05

    申请号:US11431730

    申请日:2006-05-10

    IPC分类号: C07D215/14 C07D215/12

    CPC分类号: C07D215/18

    摘要: The present invention provides a process for stereoselectively reducing 2-[3-[3-[2-(7-chloro-2-quinolinyl)ethenyl]-phenyl]-3-oxopropyyl]benzoic-acid methyl ester, to produce to produce methyl 2-[3-(S)-[3-[2-(7-chloro-2-quinolinyl)-ethenyl]phenyl]-3-hydroxypropyl]benzoate, and a process for producing montelukast or a salt thereof. The present invention further provides a process for purifying methyl 2-[3-(S)-[3-[2-(7-chloro-2-quinolinyl)-ethenyl]phenyl]-3-hydroxypropyl]benzoate. The reduction process of the present invention uses a chiral reagent and can produce the desired reduction product in high enantiomeric excess (ee).

    摘要翻译: 本发明提供了一种立体选择性还原2- [3- [3- [2-(7-氯-2-喹啉基)乙烯基] - 苯基] -3-氧代丙基]苯甲酸甲酯的方法, 2- [3-(S) - [3- [2-(7-氯-2-喹啉基) - 乙烯基]苯基] -3-羟基丙基]苯甲酸酯,以及制备孟鲁司特或其盐的方法。 本发明还提供了2- [3-(S) - [3- [2-(7-氯-2-喹啉基) - 乙烯基]苯基] -3-羟丙基]苯甲酸甲酯的纯化方法。 本发明的还原方法使用手性试剂,并且可以以高对映异构体过量(ee)产生所需的还原产物。