“一锅法”Mannich反应合成磺胺甲噁唑衍生物的研究

Study on Synthesis of Sulfamethoxazole Derivatives by Mannich Reaction in One Pot

室温条件下,以磺胺甲噁唑、苯乙酮和苯甲醛为原料,筛选反应溶剂和催化剂,获得最优反应条件:无水乙醇作为溶剂,离子液体IL 2为催化剂。在最优反应条件下进行底物拓展,制备了9种不同取代的磺胺甲噁唑衍生物,产率达到60%~94%。该合成方法条件温和,操作简便,为磺胺甲噁唑类化合物在医药领域的进一步应用提供了一定理论基础。

At room temperature,the reaction solvent and catalyst were screened with sulfamethoxazole,acetophenone and benzaldehyde as raw materials to obtain the optimal reaction conditions:absolute ethanol as the solvent and ionic liquid IL 2 as the catalyst.Under the optimal reaction conditions,nine different substituted sulfamethoxazole derivatives were prepared with yields of 60%~94%.The synthesis method was mild and easy to operate,which provided a certain theoretical basis for the further application of sulfamethoxazole compounds in the medical field.