O,O'-二烷基-α-(取代苯并噻唑-2-基)氨基-(取代苯基甲基)膦酸酯的合成与抗烟草花叶病毒活性

Synthesis and Anti-Tobacco Mosaic Virus Activity of O,O'-Dialkyl-α-(substituted benzothiazol-2-yl)amino-(substituted phenylmethyl)phosphonate

采用无溶剂无催化剂合成方法,分别进行了以O,O'-二烷基亚磷酸酯、3,4,5-三甲氧基苯甲醛、2-氨基取代苯并噻唑为原料的类Mannich一锅法合成反应研究,经合成筛选,优选出控制反应温度100℃,无溶剂、无催化剂加热反应120min的合成方法,实验结果表明该方法经济、简便、对环境友好.经元素分析,IR,1HNMR,13CNMR对所合成的化合物进行了结构确认和表征.培养并测定了化合物4a的晶体结构.初步生物活性测试表明,化合物具有一定的抗烟草花叶病毒活性.

The Mannich-type addition of O,O＇-dialkyphosphite to 3,4,5-trimethoxybenzaldehyde and 2-aminobenzothiazole was carried out in one pot by means of adopting solvent-catalyst free condition. The optimized condition is at 100 ℃ and 120 rain without catalyst and solvent, which is economic, convenient, high yields and environment-friendly. Their structures were clearly established by elemental analysis, IR, ^1H NMR and ^13C NMR spectra. Single crystals of 4a have been obtained and determined. The bioassay of some compounds showed that they have moderate anti-tobacco mosaic virus （TMV） activity.