α,α-二苯基-4-哌啶甲醇的合成研究

Study on Synthesis of α,α-Diphenyl-4-piperidinemethanol

合成了非索非那定关键中间体α,α-二苯基-4-哌啶甲醇(1)。以4-哌啶甲酸(2)、氯化亚砜和乙醇为起始原料,经酯化反应、N-保护、格氏反应及催化去保护得到1。产品含量达99%(GC),总收率为80.85%,其结构经1H NMR和IR确证。

α,α-Diphenyl-4-piperidinemethanol,a key intermediate of Fexofenadine,was synthesized from 4-piperidinecarboxylic acid,thionyl chloride and ethanol by esterification,benzylation,Grignard reaction and de-benzylation.The overall yield was 80.85%.The product structure was confirmed by 1H NMR and IR.