丁酸氯维地平合成研究进展

Research Progress in Synthesis of Clevidipine Butyrate

目的为简化丁酸氯维地平的合成步骤,优化合成路线,节约反应时间,降低工业成本提供参考.方法通过查找文献,对丁酸氯维地平的合成方法进行综述.结果丁酸氯维地平合成中所需的中间体4-(2,3-二氯苯基)-1,4-二氢-2,6-二甲基-3,5-吡啶二羧酸酯,它是通过Hantzsch法来制备的,然后再对所得中间体的侧链进行改造和修饰,本文系统地总结了以此为基础的三种合成方法,并探讨了其优缺点,以及独立于此之外新的合成方法.结论通过相关文献报道的合成方法总结梳理了氯维地平合成的研究进展,总结出满足于工业化生产要求的降低成本提高收率的丁酸氯维地平的合成方法.

Objective To provide a reference for simplifying the synthesis steps of clevidipine butyrate,optimizing the synthesis route,saving reaction time,and reducing industrial costs.Methods The literature reviewed the synthesis method of clevidipine butyrate.Results 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate,an intermediate required for the synthesis of clevidipine butyrate.It is prepared by the Hantzsch method,and then the side chain of the obtained intermediate is modified.This paper systematically summarizes three synthetic methods based on this,and discusses their advantages and disadvantages,as well as independent new synthesis methods.Conclusion The research progress of the synthesis of clevidipine is summarized through the synthesis methods reported in related literatures,and the synthesis method of clevidipine butyrate which meets the requirements of industrial production and reduces the cost and improves the yield is summarized.