含有单取代嘧啶的新型磺酰脲类化合物的设计、合成及除草活性

Design,Synthesis and Herbicidal Activity of Novel Sulfonylureas Containing Monosubstituted Pyrimidine Moiety

为了寻找高效的磺酰脲类除草剂,以商品化磺酰脲类除草剂为基础,将单取代嘧啶结构引入到分子中,合成了一系列新型磺酰脲类化合物,并通过1H NMR和高分辨质谱确定了其结构.采用盆栽法和平皿法测试了所有化合物的除草活性以及部分化合物对油菜的IC50值.结果表明,一些化合物具有一定的除草活性,其中化合物7b和7d对油菜和反枝苋具有较好的抑制活性.

Sulfonylureas,a unique group of herbicides,were extensively applied to controlling a range of weeds in a variety of crops and vegetables.In order to find efficient sulfonylurea herbicides,the title compounds were designed by introducing monosubstituted pyrimidinamines into some well-known sulfonylurea skeletons.A series of sulfonylurea compounds were synthesized and characterized by 1H NMR and HRMS.Herbicidal activities and IC50 values of the title compounds were determined by Pot plant test and Petri dish test against Brassica napus,Amaranthus retroflexus,Echinochloa crusgalli and Digitaria adscendens.Some compounds exhibited herbicidal activities.Compounds 7b and 7d possessed significant inhibition effects against Brassica napus and Amaranthus retroflexus.Further structural modification of novel sulfonylureas containing monosubstituted pyrimidine moiety will be required for improving efficacy against weeds in our lab.