比拉斯汀重要中间体的合成

Synthesis of the Key Intermediate of Bilastine

1-Boc-4-哌啶甲醇发生氧化反应得1-Boc-哌啶-4-甲醛,与2-硝基苯胺发生还原-闭环反应得4-(1H-苯并[d]咪唑-2-基)哌啶-1-羧酸叔丁酯,与2-氯乙基乙醚发生烷基化反应,再经水解得合成比拉斯汀的重要中间体1-(2-乙氧基-乙基)-2-哌啶-4-基-1H-苯并咪唑,总收率约73%。

1-Boc-piperidine-4-carboxaldehyde was prepared from 1-Boc-4-piperidinemethanol via oxidation, then it reacted with 2-nitroaniline to afford tert-butyl 4-（1H-benzimidazol-2-yl）piperidine-l-carboxylate by reductioncyclization, the latter reacted with 2-chloroethyl ethyl ether followed by hydrolysis to give the key intermediate of bilastine, 1- （2-ethoxyethyl） -2-piperidin-4-yl-benzimidazole, with a total yield of about 73 %.