摘 要：目的 研究短效二氫吡啶類鈣通道阻滯劑——丁酸氯維地平的合成工藝。方法 雙乙烯酮和3-羥基丙腈經(jīng)加成、胺化、然后與2,3-二氯亞芐基乙酰乙酸甲酯閉環(huán)縮合、水解，最后與正丁酸氯甲酯反應(yīng)制得丁酸氯維地平。結(jié)果 本工藝所得丁酸氯維地平總收率約為48%。結(jié)論 本合成工藝穩(wěn)定，條件溫和，操作簡(jiǎn)便，適合丁酸氯維地平工業(yè)化生產(chǎn)。

Abstract：Objective The process for synthesis of clevidipine butyrate (a short-acting dihydropyridine calcium channel blocker) was studied. Methods It was synthesized from diketene and 3-hydroxypropionitrile by cycloaddition and amination, then coupled with methyl 2-(2,3-dichlorobenzylidine) acetoacetate by cyc1ocondensation and hydrolysis, finally reacted with chloromethyl butyrate to give desired clevidipine butyrate. Results The overall yield of clevidipine butyrate was 48%. Conclusion The synthesis technology of clevidipine butyrate has more advantages such as stable process, mild reaction condition, and simple operation, and suitable for industrial production.