Synthesis of N,N-dimethyl-3-(4-methyl) benzoyl propionamide a key intermediate of zolpidem
    21.
    发明授权
    Synthesis of N,N-dimethyl-3-(4-methyl) benzoyl propionamide a key intermediate of zolpidem 失效
    合成N,N-二甲基-3-(4-甲基)苯甲酰基丙酰胺是唑吡旦的关键中间体

    公开(公告)号:US06921839B2

    公开(公告)日:2005-07-26

    申请号:US10363377

    申请日:2001-08-28

    CPC classification number: C07D471/04 C07C231/02 C07C235/78

    Abstract: The present invention relates to an improved and industrially advantageous process for the preparation of N,N-dimethyl-3-(4-methyl)benzoyl propionamide of Formula I, which is a key intermediate in the synthesis of zolpidem hemitartrate, a non-benzodiazepine hypnotic agent. The process includes reacting 3-(4-methyl)-benzoyl propionic acid of Formula IV, with alkyl chloroformate or pivaloyl chloride to get a mixed anhydride of Formula V; and reacting the mixed anhydride of Formula V with dimethylamine of Formula VI to get the N,N-dimethyl-3-(4-methyl)benzoyl propionamide of Formula I.

    Abstract translation: 本发明涉及用于制备式I的N,N-二甲基-3-(4-甲基)苯甲酰基丙酰胺的改进和工业上有利的方法,其是合成灭丹霉素酒渣酸盐,非苯并二氮杂的关键中间体 催眠药。 该方法包括使式IV的3-(4-甲基) - 苯甲酰基丙酸与氯甲酸烷基酯或新戊酰氯反应,得到式V的混合酸酐; 并使式V的混合酸与式VI的二甲胺反应得到式I的N,N-二甲基-3-(4-甲基)苯甲酰基丙酰胺。

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