摘要
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.
出处
《精细化工中间体》
CAS
2010年第4期34-35,37,共3页
Fine Chemical Intermediates
关键词
利培酮
4-哌啶甲酸
傅-克反应
工艺改进
Risperidone
piperidine-4-carboxylic acid
Friedel-crafts acylation
process improvement