2-甲基-6-氯苯基磺酰脲衍生物的合成及生物活性  

Synthesis and Biological Activity of 2-Methyl-6-chlorobenzenesulfonylurea Derivatives

作　　者：陈伟[1] 魏巍[1] 吴长春[1] 李玉新[1] 李永红[1] 于淑晶[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化学化工协同创新中心(天津),天津300071

出　　处：《有机化学》2015年第7期1576-1581,共6页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.21272129);国家科技部科技支撑计划(No.2011BAE06B05)资助项目~~

摘　　要：为探索磺酰脲类化合物的生物活性多样性,以商品化磺酰脲除草剂为基础,设计并合成了12个未见文献报道的2-甲基-6-氯苯基磺酰脲衍生物,通过1H NMR,13C NMR和HRMS确定了其结构.经盆栽法除草测试表明,目标化合物对双子叶靶标油菜和反枝苋具有优异的的除草活性,如5b,5i和5j对油菜和稗草的除草活性与氯磺隆和单嘧磺隆相当.离体抑菌实验表明,在50 mg·L-1剂量下,部分化合物对所测试植物性病菌具有不错的抑菌活性.In order to study the multi-bioactivity of sulfonylurea （SU） derivatives, twelve novel 2-methyl-6-chlorobenzenesul- fonylureas were designed and synthesized according to the commercialized SUs skeletons. Their structures were confirmed by 1H NMR, 13C NMR and HRMS. The title compounds showed good herbicidal activity against dicotyledonous weeds by pot-culture method. For example, the herbicidal activity of 5b, 5i and 5j against Brassiea napus, Amaranthus retroflexus was as effective as chlorsulfuron and monosulfuron. The in vitro antifungal test indicated that some of the target compounds exhibited good antifungal activity at the dosage of 50 mg.L-1.

关 键 词：磺酰脲 氯磺隆 除草活性 抑菌活性 

分 类 号：TQ457.2[化学工程—农药化工]