摘 要：目的 研究適合工業(yè)化生產(chǎn)的丁酸氯維地平合成方法。方法 采用2,3-二氯苯甲醛、β-氨基巴豆酸甲酯與乙酰乙酸乙酯環(huán)化縮合，選擇性水解得到4-(2,3-二氯苯基)-1,4-二氫-2,6-二甲基-3,5-吡啶二羧酸單甲酯鉀鹽，再同丁酸氯甲酯反應(yīng)得到丁酸氯維地平。結(jié)果 該合成工藝的丁酸氯維地平總收率為48%。結(jié)論 該工藝穩(wěn)定，操作簡(jiǎn)單，適合工業(yè)化生產(chǎn)丁酸氯維地平。

Abstract: Objective To investigate the industrialization method for clevidipine butyrate．Methods Clevidipine butyrate was synthesized after several processes，including cyclocondation of 2,3-dichlorobenzalde- hyde，methyl β-aminobutenate and ethyl acetoacetate，selective hydrolysis through which 4-(2,3-dichloro- pheny1)-1,4-dihydro-2,6-dimethy-3,5-pyridinedicarboxylic acid monomethyl ester potassium salt was obtained，and reaction with chloromethy butyrate．Results The total yeild rate of clevidipine butyrate was 48%．Conclusion This method was simple and reproducible，and this synthesis route is suitable for the commercial production of clevidipine butyrate．