2-噻唑烷酮磺酰脲衍生物的合成及生物活性  

Synthesis and biological activity of novel 2-thiazolidiones sulfonylurea derivatives

作　　者：陈庆悟[1] 沈德隆[1] 

机构地区：[1]浙江工业大学化材学院,浙江杭州310032

出　　处：《浙江工业大学学报》2008年第5期562-564,共3页Journal of Zhejiang University of Technology

摘　　要：磺酰脲类除草剂是一类超高效、广谱、对哺乳动物低毒和高选择性的除草剂.2-噻唑烷酮可直接用作杀菌剂、杀虫剂、植物生长调节剂.磺酰脲类除草剂的残留以及对后茬作物的毒性成为它进一步发展的一个重要制约因素.为发现新的先导化合物,以2-噻唑烷酮,单取代苯磺酰胺,草酰氯为原料,通过异氰酸酯法合成了5个未见报道的磺酰脲衍生物,结构经NMR,IR,MS确定.初步测定了这些化合物的生物活性,5个化合物均无杀虫,杀菌活性,一种化合物显示了良好的除草活性,100 mg/L浓度下,对单子叶植物-稗草根的抑制率为91.1%.The sulfonylurea herbicides are a kind of weed control agents characterized by broad- spectrum, ultralow dosage, good crop selectivity and low mammalian toxicity. 2-Thiazolidiones can be used directly as fungicide, insecticide and plant growth regulator. The phototoxicity of sulfonylurea herbicides residues to succeeding crops has become one of important factors affecting its further development. In order to search for some new lead compounds, using 2-thiazolidiones, mono-substituent benzenesulfonamide and oxaiyl chloride as starting materials, five new derivatives were synthesized from isocynate. The structures of these compounds were confirmed by NMR, IR, MS. Preliminary bioassays indicated that all compounds possessed no fungicidal and insecticidal activity. Only one new compound exhibited good herbicidal activity. The inhibition rate was 91.1% at 100 mg/L against the root of Echinochloa Crusgalli.

关 键 词：磺酰脲 2-噻唑烷酮 磺酰异氰酸酯 生物活性 

分 类 号：O626.21[理学—有机化学]