绿色水油兼溶的除草剂的设计、合成与生物活性研究  

Design,synthesis and bioactivity evaluation of novel herbicides with water and oil soluble

作　　者：邹小毛[1,2] 刘殿甲[1] 傅翠蓉[1] 李永红[1] 

机构地区：[1]元素有机化学国家重点实验室,南开大学元素有机化学研究所,天津300071 [2]天津化学化工协同创新中心,天津300071

出　　处：《中国科学：化学》2016年第11期1226-1234,共9页SCIENTIA SINICA Chimica

基　　金：国家自然科学基金(编号:211721230;21472102)资助项目

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.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.

关 键 词：水油兼溶 APP类除草剂 精喹禾灵 氰氟草酯 绿草定 ACC酶 

分 类 号：TQ457.2[化学工程—农药化工]