N-(4'-取代嘧啶-2'-基)-2-甲氧羰基-5-(取代)苯甲酰胺基苯磺酰脲化合物的合成及除草活性研究

Synthesis and Herbicidal Activity of N-(4'-Substituted pyrimidin-2'-yl)- 2-methoxycarbonyl-5-[(un)substituted benzamido]phenyl- sulfonylurea Derivatives

为进一步寻找高效、安全和对环境更加友好的除草剂,以商品化除草剂单嘧磺酯为研究基础,对其结构中的苯环5-位取代基作了结构修饰,合成了26个未见文献报道的新型N-(4'-取代嘧啶-2'-基)-2-甲氧羰基-5-苯甲酰胺基苯磺酰脲化合物,通过1HNMR、质谱及元素分析确定了化合物的结构.经油菜平皿法及盆栽法测试了所有化合物的除草活性,结果表明,当苯环5-位取代基为苯甲酰胺时,活性较好,其对双子叶植物的除草活性与商品化的甲嘧磺隆相当.

In order to search for ecologically-safer and environmentally-benign sulfonylurea herbicides, on the basis of study on the N-（4-methylpyrimidin-2-yl）-N＇（2-methoxycarbonyl phenylsulfonyl）urea, named monosulfuron, a commercialized herbicide invented by our laboratory, 26 novel benzenesulfonylurea compounds modified at the 5-position of the benzene ring were synthesized. The structures of all compounds synthesized were confirmed by elemental analysis, MS and ^1H NMR spectra. Herbicidal activity of the new compounds was determined by rape disc and pot bioassay experiments. The result indicated that when the substituent group at 5-position of the benzene ring was benzamide, the herbicidal activity was good compared to sulfometuron-methyl.