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

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。

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

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-triazolo3,4-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.