新型含三唑啉酮的磺酰脲类化合物的合成、晶体结构及除草活性研究  

Synthesis, Crystal Structure and Herbicidal Activity of Novel Sulfonylureas Containing Triazolinone Moiety

作　　者：潘里[1] 陈有为[1] 刘卓[1] 李永红[1] 李正名[1] 

机构地区：[1]南开大学元素有机化学研究所元素有机化学国家重点实验室,天津300071

出　　处：《有机化学》2013年第3期542-550,共9页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.21272129);国家重点基础研究发展计划(973;No.2010CB126106);国家科技攻关计划(No.2011BAE06B05)资助项目~~

摘　　要：为了进一步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,将三唑啉酮杂环引入到分子中,合成了23个未见文献报道的新型磺酰脲化合物,通过1H NMR、高分辨质谱以及X射线单晶衍射确定了其结构.经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,化合物5h具有优秀的除草活性,其对油菜的IC50值与对照药醚苯磺隆和醚磺隆相近,在3.75 g/ha浓度下对单子叶杂草稗草具有优异的盆栽抑制活性.In order to search for efficient sulfonylurea herbicides, the title compounds were designed by introducing triazoli- nones into some known sulfonylurea structures. 23 novel sulfonylurea compounds had been synthesized and characterized by 1H NMR, HRMS and X-ray diffraction. Herbicidal activities of title compounds were determined by pot-culture method. IC50 values of some effective sulfonylurea compounds were tested by culture dish method. It was found that compound 5h attained the super-active level which was comparable to the controls as triasulfuron and cinosulfuron. It was worthy to note that com- pound 5h had potent inhibitory activity against Echinochloa crusgalli by pot-culture method at 3.75 g/ha.

关 键 词：磺酰脲 三唑啉酮 合成 晶体结构 除草活性 

分 类 号：TQ457.2[化学工程—农药化工]