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目的对西格列汀的合成工艺进行改进。方法以2,4,5-三氟苯乙酸为原料,经亲核取代、环化、氢化、Na BH4还原反应,并进行拆分优化。结果制得的西格列汀光学纯度高于98%、总收率36%。结论拆分方法具有操作简便、生产成本低、反应条件温和的优点,适用于西格列汀的工业化应用。
Objective To improve the synthesis of sitagliptin. Methods 2,4,5-trifluorophenylacetic acid was used as a starting material, followed by nucleophilic substitution, cyclization, hydrogenation and Na BH4 reduction, and its resolution was optimized. Results The obtained sitagliptin had an optical purity higher than 98% and a total yield of 36%. Conclusion The resolution method has the advantages of simple operation, low production cost and mild reaction conditions, and is suitable for the industrialized application of sitagliptin.