2,4-二氟苯基-4-哌啶基甲酮盐酸盐的合成工艺研究

Research on the Synthesis of (2,4-Difluorophenyl) (piperidin-4-yl)methanone Hydrochloride

以4-哌啶甲酸、氯甲酸乙酯为原料,经酰胺化、傅-克酰基化反应、水解得到2,4-二氟苯基-4-哌啶基甲酮盐酸盐(4),总收率为62.4%。该法原料易得、操作简便、收率高,各主要化合物结构经核磁共振氢谱确证。

Piperidine-4-carboxylic acid and ethyl carbonochloridate were used as the starting materials for preparation of（2,4-difluorophenyl）（piperidin-4-yl）methanone hydrochloride（4） via amidation,Friedel-crafts acylation and hydration.The staring materials were easily available and the process afforded a reasonable overall yield of 62.4%.The structures of the intermediates and the target compound were identified with 1H NMR.