利多卡因由2，6-二甲基苯胺先经氯乙酰氯酰化、再经二乙胺胺化两步工艺路线制得。在不加入催化剂的情况下，第2步胺化反应的自然反应时间在8 h以上，耗时太长。通过改变第2步的反应溶剂、底物之间的摩尔比、催化剂和温度等优化反应工艺。结果表明，反应溶剂为乙腈、底物n（N-氯乙酰-2，6-二甲基苯胺）∶n（二乙胺）=1∶2、催化剂为无水碳酸钾1.0 eq+碘化钾0.1 eq、温度为55~70℃时，反应时间缩短了4 h，产品利多卡因摩尔收率达到85.17%，产品纯度达到99.777%。

Lidocaine is prepared from 2, 6-dimethylaniline by chloroacetyl chlorination at first and then diethylamine amination.Without catalyst, the natural reaction time of amination in the second step spends more than 8 hours.The reaction process is optimized by changing the reaction solvent, the molar ratio between substrates, catalyst and temperature in the second step.The results show that the reaction time is shortened by 4 hours, the molar yield of lidocaine reaches 85.17% and the product purity reaches 99.777% when acetonitrile is served as the reaction solvent, n(N-chloroacetyl-2, 6-dimethylaniline):n(diethylamine)=1:2, the temperature is 55-70℃, and anhydrous potassium carbonate 1.0 eq+ potassium iodide 0.1 eq is used as the catalyst.

刘畅畅(1996-),男,硕士研究生,研究方向为生物与医药,1285896631@qq.com