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哌嗪经2-氯嘧啶进行单烃化得到2-(1-哌嗪基)嘧啶(3)。另用1,2-亚甲二氧基苯经Blanc氯甲基化反应得到胡椒基氯(2)。2与3进行烃化反应制得帕金森病治疗药吡贝地尔,总收率约64%(以2-氯嘧啶计)。
Piperazine was mono-alkylated with 2-chloropyrimidine to give 2- (1-piperazinyl) pyrimidine (3). In addition, 1,2-methylenedioxybenzene was subjected to Blanc chloromethylation to obtain piperonyl chloride (2). 2 and 3 were alkylated to produce Parkinson’s disease drug piribedil. The total yield was about 64% (based on 2-chloropyrimidine).