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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-4-piperidinemethanol was oxidized to give 1-Boc-piperidine-4-carbaldehyde by reduction-ring closure with 2-nitroaniline to give 4- (1H-benzo [d] Yl) piperidine-1-carboxylate was alkylated with 2-chloroethylether and then hydrolyzed to synthesize 1- (2-ethoxy-ethyl ) -2-piperidin-4-yl-1H-benzimidazole in a total yield of about 73%.