那格列奈H晶型的合成

Synthesis of Nateglinide

目的:以反-4-异丙基环己基甲酸、氯化亚砜、D-苯丙氨酸为原料制备那格列奈B型晶,再转为H型晶。方法:通过改变反应温度、时间,溶剂等条件来完成那格列奈H晶型的制备。结果:目标产物那格列奈H型晶制备总收率为60%。结论:该合成路线终产品纯度、收率均有所提高,且转晶完全,操作简便适合工业化生产。

Objectie. To improve the synthesis technology of Nateglinide. Method： The B crystal form of Nateglinide was prepared from trans-4-isopropyeyclohexane carboxylic acid and D-phenylalanine and then was transformed to its H crystal form. The H crystal form of Nateglinide was prepared by changing the reaction conditions such as temperature, time and solvent. Results： The B crystal form of Nateglinide was synthesized with an overall yield of 60%. Conclusion： The improved synthesis technology The improved synthesis technology has many advantages,such as more convenient operation ,lower cost , higher yield, suithle for its industrialized production.