微波辅助双水杨酰肼的高效制备及其HIV抑制活性研究(英文)

Microwave-Induced Rapid Preparation of N,N′-Disalicylhydrazine and Its Anti-HIV Activity

以水杨酸甲酯(1)为原料,微波辅助的无溶剂反应为关键步骤,实现了双水杨酰肼(2)的高效合成。经过实验尝试,确定优化反应条件为:微波功率100 W,反应温度150℃,封管反应1 h,收率77%。化合物结构经熔点、1H NMR和元素分析确证。生物活性研究发现双水杨酰肼(2)具有HIV抑制活性。

A novel and efficient method for the preparation of N,N＇-disalicylhydrazine（2） under microwave irradiation and in solvent-free conditions has been accomplished starting from methyl salicylate （1）. The reaction was carfled out under 100 W, 150℃ in sealed-tube for 1 hour, affording the N,N＇-disalicylhydrazine （2） in 77% yield. The product structure was characterized by melting point, 1^H NMR spectrum and elemental analysis. The bioassay results indicated that the compound N,N＇-disalicylhydrazine（2） possess anti-HIV activity.