N-氰基-N′-取代芳甲基脒基膦酸酯类化合物的合成及其生物活性

Synthesis and Biological Activity of N-cyano-N′-arylmethyl Carbamimidoyl Phosphonate

N-氰基-S,S-二甲基二硫代碳酸酯在THF中与亚膦酸二烷基酯的钠盐反应得到中间体;再与多种芳甲胺反应合成了九个未见文献报导的N-氰基-N′-取代芳甲基脒基膦酸酯类化合物(3a^3i),其结构经1H NMR,31P NMR,HR-MS或元素分析表征。初步生物活性测试结果表明,当用药浓度为10 ppm时,3对黄瓜子叶生根具有一定的促进作用,对蚜虫和红蜘蛛没有抑制活性。

Nine novel N-cyano-N＇-arylmethyl carbarnimidoyl phosphonates（3a - 3i） were synthesized through the reaction of various arylmethyl amines with N-cyanoimido-phosphonyl/S-methyl thiocarbonates at room temperature. The structures were characterized by ^1H NMR, ^31p NMR, HR-MS or elemental analysis. Preliminary bioassay indicated that some of 3 stimulated certain radicle growth of cucumber at 10 ppm.