1,4-苯基双氨基膦酸酯的绿色合成及生物活性

Green Synthesis and Fungicidal Activity of 1,4-Phenyl Bisaminophosphonates

在不加任何溶剂和催化剂条件下,通过微波辅助一锅法合成了9种1,4-苯基双氨基膦酸酯。该反应时间短(4～6min),后处理简单,环境友好,产率达到85%～95%,是一种高效绿色的合成方法。通过1HNMR、13 C NMR和元素分析确定了目标化合物的结构。生物活性测试表明,该类化合物对革兰氏阳性菌(金黄色葡萄球菌)有很好的抑菌活性。

Nine kinds of 1,4-phenyl bisaminophosphonates were synthesized efficiently by microwave-assisted three-component Kabachnik-fields reaction with solvent-free and catalyst-free method with 85% ～ 95% yields. Thereactions exhibited the advantages of short reaction time （ only 4 ～ 6min ） and green synthesis. The chemical structures of the as-synthesized phosphonates were confirmed by 1 H NMR,13 C NMR and elemental analysis. Their biological tests indicated they have better sterilizing activity for gram-positive bacterium （staphylococcus aureus）.