拉奎莫德的合成工艺优化

摘要

Objective To synthesize Laquinimod and optimize the synthetic technology . Methods Taking 2-amino-6-ehlorobenzoic acid as raw material, Laquinimod was synthesized by a series of chemical reactions including cyclization , methylation, condensation, and amida-tion. Results Laquinimod was prepared with an overall rate of 77. 8%. Conclusion The improved procedure could simplify the synthe -sis,reduce the cost and improve the yield.%目的 分析比较拉奎莫德的合成方法并且进行工艺优化.方法 以2-氨基-6-氯苯甲酸为起始原料与氯甲酸苄酯、乙酰氯进行环合反应,再经甲基化、缩合、酰胺化反应制得拉奎莫德.结论 合成的拉奎莫德的总收率为77.8%,纯度为99.1%.其结构经1H-NMR和MS确证.结论工艺改进后,操作简化,成本降低,收率提高,适合工业化生产.