【摘要】 本文选取了芳氧苯氧丙酸酯类除草剂精喹禾灵、氰氟草酯及吡啶类除草剂绿草定为先导化合物,在-研究它们的构效关系、作用机制和吸收传导规律的基础上,将药效基团N,N-二取代乙醇胺或N,N-二取代乙二胺引入其结构中,设计合成了精喹禾灵和氰氟草酯衍生物及绿草定衍生物(C、E两个系列)共30个新颖结构的化合物,以期开发出具有水油兼溶的高活性除草剂分子.结果显示,大多数化合物的盐酸盐水溶性很好,可以直接用水作溶剂进行生物活性测试.生物活性测试表明,C-4和C-9在施用量0.4 g/亩时对稗草的抑制活性达100%,略优于商品化的精喹禾灵;E-6在施用量20 g/亩时对稗草的抑制活性为70%,为绿草定活性的3倍多.更多还原

【Abstract】 For finding high effective herbicides with water and oil soluble that can be directly utilized in aqueous agent, 30 compounds with Quizalofop-p-ethyl, Cyhalofop-butyl or Triclopyr as skeleton and containing N,N-disubstituted ethanolamine or N,N-disubstituted ethanediamine were synthesized. These compounds are classified two series series C and E. Their structures were characterized by elemental analyses, ¹H NMR, ¹³ C NMR, HRMS and IR. Their bioactivities were also tested. In the bioassays, Quizalofop-p-ethyl derivatives C-4 and C-9 showed excellent bioactivity; Cyhalofop-butyl derivatives exhibited certain herbicidal activity; Compound E-6 demonstrated 70% inhibition of Echinochloa crus-galli in 300 g a.i./ha which is more than 3 times as that of Triclopyr. Moreover, One third of the derivatives can be water and oil soluble.更多还原