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1,2,4-三唑并[3,4-b]-1,3,4-噻二唑的合成、结构及生物活性

Synthesis,structure and biological activity of 1,2,4-triazolo [3,4-b]-1,3,4-thiadiazole

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【作者】 靳如意孙晓红刘源发陆文婷杨清翠

【Author】 JIN Ru-yi1,SUN Xiao-hong1,2,LIU Yuan-fa3,LU Wen-ting1,YANG Qing-cui1(1.School of Chemical Engineering;2.Chemical Research Institute;3.School of Chemistry & Materials Science,Northwest University,Xi’an 710069,Shaanxi Province,China)

【机构】 西北大学化工学院西北大学化学研究所西北大学化学与材料科学学院

【摘要】 为了筛选出新的高活性化合物,以二氨基硫脲与有机羧酸为原料,回流反应生成中间体4-氨基-5-取代-1,2,4-三唑硫酮,再与羧酸在POCl3的催化下合成了3,6-双取代1,2,4-三唑并[3,4-b]-1,3,4-噻二唑新化合物。目标化合物通过IR、元素分析和1H NMR对其结构进行了表征。并初步测定了该化合物对5种植物病原菌(烟草赤星病、马铃薯干腐病、小麦赤霉病、番茄早疫病、西瓜枯萎病)的杀菌活性,结果表明此类化合物对所测菌种具有良好的杀菌、抑菌作用。

【Abstract】 In order to screen out the novel highly-active compounds,the intermediate 4-amino-5-substituted-1,2,4triazolethione was synthesized by using thiocarbohydrazide and carboxylic acids as raw materials,and then the new compounds of 3,6-disubstituted-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole were synthesized by the intermediates 4amino-3-mercapto-5-substituted-1,2,4-triazole with carboxylic acids in the presence of phosphorus oxychloride as catalyst.The structures of target compounds were characterized by IR,elemental analysis and 1 H NMR.Their preliminary biological activities to five vegetable pathogens(including Gibberlla nicotiancola,Pythium solani,Gibberlla saubinetii,Alternaria iycopersici and Fusarium oxysporium f.s.p.niveum) were tested.The results show that most of them exhibit good fungicidal activities.

【关键词】 1,2,4-三唑合成噻二唑生物活性
【Key words】 1,2,4-triazolesynthesisthiadiazolebiological activity
【基金】 国家自然科学基金资助项目(21073141);西北大学研究生创新基金资助项目(10YZZ32)
  • 【文献出处】 化学工程 ,Chemical Engineering(China) , 编辑部邮箱 ,2013年01期
  • 【分类号】O626.2
  • 【被引频次】2
  • 【下载频次】223
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