6-N-取代的2,4,8,10-四氯-6-硫-12H-双苯并  -二氧磷杂八环的合成及杀菌活性

Synthesis and Fungicidal Activity of 6-N-Substituted 12H-1,3,2-diozaphosphorcin-6-sulfoxides

摘要: 通过2,4,6,8,10-五氯-6-硫-12H-双苯并二氧磷杂八环分别与四氢吡咯、六氢吡啶、吗啉、吡咯、咪唑和1,2,4-三唑反应,得到了6个收率良好的标题新化合物。其结构经1H、13C、31P NMR和元素分析确认。初步杀菌活性测定表明,化合物 3c和3d 在500 μg/mL浓度下对水稻纹枯病菌Pellicularia sasakii的抑制率为48%~50%,其他化合物对供试菌的活性微弱。

Abstract: Six novel compounds were synthesized in high yields by the reaction of 2,4,6,8,10-pentachloro-12H- -diozaphosphorcin-6-sulfoxide with tetrahydropyrrole,piperidine,morpholine,pyrrole,imidazole,and 1,2,4-triazole,respectively.Their structures were confirmed by elementary analysis, 1H, 13C,and 31P NMR data. Preliminary bioassay results showed that 3c and 3d have moderate inhibition rate(48% ~50%)against Pellicularia sasakii at 500 μg/mL. Other compounds showed week inhibition effects against the tested fungi.