含噻唑、硫醚结构的1,2,4-三唑类化合物的合成及生物活性  

Synthesis and Bioactivity of New 1,2,4-Triazole Compounds Containing Thiazole and Thioether

作　　者：钱存卫[1] 黄海军 费正皓[1] 张愉晴 王栋[1] 宗乾收[3] 

机构地区：[1]盐城师范学院化学化工学院,江苏盐城224007 [2]盐城利民农化有限公司,江苏盐城224005 [3]嘉兴学院生物与化学工程学院,浙江嘉兴314001

出　　处：《应用化学》2015年第4期399-404,共6页Chinese Journal of Applied Chemistry

基　　金：2013年江苏省科技支撑(工业)项目基金(SBE201330457);江苏省高校自然科学基金(14JKD150009)资助~~

摘　　要：以三氟乙酰乙酸乙酯、磺酰氯、水合肼、异硫氰酸苯酯、碘代芳烃、氯乙酸等为原料,设计、合成了7种新型的含噻唑环、硫醚和三氟甲基的1,2,4-三氮唑类化合物,通过1H NMR、13C NMR、19F NMR和MS等技术手段对新化合物进行了结构表征。杀菌活性测试表明,化合物6b、6d和6g在浓度为100 mg/L时对纹枯病菌(Rhizoctoniasolani)的抑制率分别为91%、92%和93%。Seven novel 1,2, 4-triazole derivatives containing thioether and thiazole were designed and synthesized from ethyl 4, 4, 4-trifluoro-3-oxobutanoate, sulfonyl chloride, hydrazine hydrate, phenyl isothiocyanate, aryl iodides, chloroacetic acid as starting materials v/a substitution, hydrazinolysis, cyclization and Ullmann coupling. The structures of these compounds were characterized with ^13C NMR, ^1H NMR, ^19F NMR and MS. Bactericidal activity test shows that Rhizoctoniasolani can be inhibited by compounds 6b, 6d, and 6g at a concentration of 100 mg/L with inhibition rates of 91%, 92% and 93%, respectively.

关 键 词：噻唑 三氮唑 硫醚 合成 生物活性 

分 类 号：O626.2[理学—有机化学]