Based on 2-cyanoacetamide as raw material, fourteen 5-pyrimidinyl-1, 2, 4-oxadiazole derivatives were synthesized through four step reactions including condensation, cyclization, aminolysis and cyclization.The structures of these compounds were characterized by 1H NMR, 13C NMR, MS and elemental analysis.The antifungal activity of them against eight phytopathogens were tested by the linear growth rate method at the concentration of 50 μg·mL-1.The results showed that most target compounds exhibited moderate fungicidal activity.Among of them, 4 k showed the highest activity and its inhibition rate against phomopsis sp.was 84.57%, which was equivalent to pyrimethanil.%以氰基乙酰胺为原料, 经过缩合、环化、氨解和环化合成14个5-嘧啶基1, 2, 4-噁二唑衍生物.通过1H NMR, 13C NMR, MS和元素分析确证其结构.采用菌丝生长速率法测定14个化合物在50μg·mL-1时对8种植物病原真菌的活性, 结果表明大部分目标产物对8种病菌具有中等抗菌活性.其中4k对猕猴桃拟茎点霉菌 (Phomopsis sp.) 抑制率与商品药剂嘧霉胺活性相当.
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