4-取代嘧啶基苯磺酰脲类化合物的合成与除草活性  

Synthesis and herbicidal activity of novel 4-substituted pyrimidinyl-phenyl-sulfonylureas

作　　者：郑占英[1] 陈建宇[1] 刘桂龙[1] 李永红[1] 李正名[1] 

机构地区：[1]南开大学元素有机化学国家重点实验室农药国家工程研究中心(天津),天津300071

出　　处：《农药学学报》2012年第6期607-611,共5页Chinese Journal of Pesticide Science

基　　金：国家重点基础研究发展计划("973"计划)项目(2010CB126106课题);"十二五"国家科技支撑计划课题(2011BAE06B05)资助

摘　　要：为了探寻磺酰脲类除草剂的构效关系,以单嘧磺隆和单嘧磺酯为先导化合物,在嘧啶环上引入取代苯基,设计合成了16个新型单取代嘧啶磺酰脲衍生物,其结构均经过核磁共振氢谱、质谱和元素分析确证。盆栽试验结果表明:在1.5 kg/hm2时,大部分化合物对供试杂草具有一定的抑制活性,其中对双子叶杂草的活性高于对单子叶杂草的活性,但均不及先导化合物的活性。Sulfonylurea herbicides,widely applied in agricultural crop protection worldwide,were a milestone of the herbicide development because of its ultra-high activity at low application rates with low toxicity and environmentally benign characteristics.In order to study further structure activity relationship of these kind of herbicides,on the basis of our former studies,16 novel 4-phenylpyrimidine sulfonylurea compounds were rationally designed and synthesized using monosulfuron and monosulfuron-ester as leads.All structures of the new compounds synthesized were confirmed by 1H NMR,MS and elemental analysis.Preliminary herbicide screening indicated that,most compounds show certain extent inhibitory activity to various weeds at 1.5 kg/hm2,the inhibitory activity to dicotyledonous weeds were better than those to monocotyledonous weeds.Phenyl substituted pyrimidines were not benefit to improvement of herbicide activity.

关 键 词：4-取代苯基嘧啶 磺酰脲 合成 除草活性 

分 类 号：O625.25[理学—有机化学]