公开(公告)号：US06921839B2

公开(公告)日：2005-07-26

申请号：US10363377

申请日：2001-08-28

Applicant: Yatendra Kumar ,  Mohan Prasad ,  Azok Nath

Inventor： Yatendra Kumar ,  Mohan Prasad ,  Azok Nath

IPC: C07C231/02 ,  C07C235/78 ,  C07D471/04

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。