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目的:确定并优化新一代抗高血压药物丁酸氯维地平的合成工艺。方法:以3-羟基丙腈和双乙烯酮为起始原料,经缩合、胺解、环合、水解、酯化等5步反应得到丁酸氯维地平。结果:通过工艺改进,革除原文献中柱层析的后处理方法,总收率33.7%,产品纯度达到99.98%。结论:本研究路线原料易得,价格低廉,反应条件温和,适合于工业化生产。
OBJECTIVE: To identify and optimize the synthesis of a new generation of anti-hypertensive drug, clevidipine butyrate. Methods: 3-Hydroxypropionitrile and diketene were used as starting materials to obtain clevidipine butyrate by five steps of condensation, amidation, cyclization, hydrolysis and esterification. Results: Through the process improvement, the post-treatment method of column chromatography in the original literature was eradicated. The total yield was 33.7% and the purity of the product reached 99.98%. Conclusion: The raw materials of this research are easy to obtain, cheap, mild reaction conditions, suitable for industrial production.