新单取代苯磺酰脲衍生物的合成及生物活性

以较高活性的单取代苯磺酰脲为基础,设计合成了14个新的含烷硫基和烷胺基嘧啶环的单取代苯磺酰脲化合物,其结构经¹HNMR及元素分析确证.用油菜根长法测定IC₅₀,并进行盆栽除草活性测试,结果表明,嘧啶环4位取代基的变化对分子除草活性影响较大,活性大致按烷氧基、烷硫基和烷胺基的顺序递减.

Synthesis and Biological Activity of New Phenylsulfonylurea Derivatives

In order to develop new herbicidal active structures and research the structure-activity relationship, on the basis of the known monosubstituted phenylsulfonylureas with a high activity we designed and synthesized 14 novel sulfonylurea compounds with a single substituting group, such as alkoxy, alkylthio and alkylamino in the pyrimidine ring. The structures of all compounds were confirmed by 1H NMR spectra data and elemental analysis. Herbicidal activitiy including IC 50 was determined by rape root length experiment and pot experiment. The results show that the variation of 4- substituting group of the pyrimidine ring affects the activity of the compounds respectively. Herbicidal activity decreases in the sequence of alkoxy, alkylthio and alkylamino substituent.