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有机化学.pdfVIP

DOI: 10.6023/cjoc201211018 研究论文 有机化学 Chinese Journal of Organic Chemistry ARTICLE 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 潘 里 陈有为 刘 卓 李永红 李正名* (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) 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. 关键词 磺酰脲; 三唑啉酮; 合成; 晶体结构; 除草活性 Synthesis, Crystal Structure and Herbicidal Activity of Novel Sulfonylureas Containing Triazolinone Moiety Pan, Li Chen, Youwei Liu, Zhuo Li, Yonghong Li, Zhengming* (Research Institute of Elemento-organic Chemistry, State Key Laboratory of Elemento-organic Chemistry, Nankai University, Tianjin 300071) Abstract 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. Keywords sulfonylurea; tr