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摘 要:目的 研究短效二氢吡啶类钙通道阻滞剂——丁酸氯维地平的合成工艺。方法 双乙烯酮和3-羟基丙腈经加成、胺化、然后与2,3-二氯亚苄基乙酰乙酸甲酯闭环缩合、水解,最后与正丁酸氯甲酯反应制得丁酸氯维地平。结果 本工艺所得丁酸氯维地平总收率约为48%。结论 本合成工艺稳定,条件温和,操作简便,适合丁酸氯维地平工业化生产。
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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.
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