目的 對西格列汀的合成工藝進行改進。方法 以2，4，5-三氟苯乙酸為原料，經(jīng)親核取代、環(huán)化、氫化、NaBH4還原反應(yīng)，并進行拆分優(yōu)化。結(jié)果 制得的西格列汀光學純度高于98%、總收率36%。結(jié)論 拆分方法具有操作簡便、生產(chǎn)成本低、反應(yīng)條件溫和的優(yōu)點，適用于西格列汀的工業(yè)化應(yīng)用。

Objective To study the improved method for synthesis of sitagliptin. Methods 2,4,5-Trifluoro phenyl acetic acid was used as raw material to synthesize the target compound by nucleophilic substitution, cyclization, hydrogenation, and NaBH4 reduction. And isomer resolution was optimized. Results After optimization, sitagliptin with optical purity of 99.7% was obtained. The total recovery of the synthetic route was 36%. Conclusion The resolution method with advantages of easy-operation, low production cost, and mild reaction conditions is suitable for industrial application of sitagliptin.