来曲唑合成工艺改进

Improvement on Synthesis of Letrozole

以对氯苯腈等物为原料,进行的各种取代反应合成实验实行改进,考察了每一反应步骤中反应温度对反应进程的影响并对反应曲线进行了解释。实验结果表明,最佳的反应温度为:合成化合物1的较佳反应温度为60℃;生成化合物2的最佳置换反应温度为55℃。第三步取代反应将反应温度用冰水浴控制在0℃。改进后的实验廉价、易操作、产率高,对工业生产及实验教学有积极的指导作用。

A promoted route to synthesizing letrozole was introduced. Using chlorobenzonitrile as reactants, the preparation of letrozole acetate was improved. The factors which influence the reactive performance of letrozole acetate were investigated and optimized, including reaction temperature of each step. The results indicate that the best reaction conditions are as follows： The temperature is 60 ~C , when synthesizing compound 1, the temperature is 55 ~C , when synthesizing compound 2, and the temperature should be controlled to 0 ~C by ice-water system, when synthesizing compound 3. The improved experiment is cheap, easy to operate, and productive. It has instructional significance for industrial production and experimental teaching.