新型强心药物匹莫苯的合成

Synthetic Studies on Pimobendan(A Positive Inotropic Agent)

以乙酰苯胺为起始原料，采用两种不同的路线合成新型强心药物匹莫苯，总收率为１８．５％．实验表明，先烷基化、后硝化制备化合物（５）的方法比由中间体（６）制备（５）的收率高，而且产物的后处理较方便．关键中间体及最终化合物的结构经元素分析、质谱、核磁共振氢谱及碳谱得到了确证．合成中避免使用毒性高的氰化钾及高压反应条件，适合于工业化生产．

Pimobendan,a new kind of positive inotropic agent,was synthesized by two noval synthetic routes.The total yield was 18 5%.The yield of compound (5) obtained from the route via alkylation first,then nitration was higher than that from the route via nitration first,then alkylation.The structures of the intermediates and target molecule were confirmed by MS,elementary analysis, 1H NMR and 13 C NMR spectrometry in our experiments.The routes without highly toxic potassium cyanide and high pressure may be applied to industrial production.