含苯并噻唑杂环的α-氨基烷基膦酸二乙酯的合成及生物活性

The Synthesis and Biological Activity of Diethyl N (2 Benzothiazolyl) α aminoalkylphosphonate

用亚磷酸二乙酯与亚胺加成的方法合成了２０个Ｎ－（２－苯并噻唑基）－α－氨基膦酸二乙酯类化合物．利用协同３＋２机理对反应进行了解释．运用量子化学方法（ＭＩＮＤＯ／３）计算了亚胺分子的原子电荷，并讨论了取代基对五元环过渡态形成的影响．所合成的部分化合物具有较好的抑制烟草花叶病毒（ＴＭＶ）活性和一定的除草活性．

Twenty diethyl N (2 benzothiazolyl) α aminoalkylphosphonates were synthesized by addition of diethyl phosphite to the corresponding imine. The reaction phenomenon was explained by a concerted 3+2 mechanism. The atomic charge of imine was calculated by quantum chemistry(MINDO/3) and the effect of substitutes on the formation of pentacyclic transition state was discussed. Some compounds showed a very good inhibitory effect against tobacco mosaic virus(TMV) and herbicidal activity.