【摘要】 用KMnO4/HOAc氧化 2 甲硫基 5 吡唑基 1,3,4 二唑 1,得到中间体 2 甲磺酰基 5 吡唑基 1,3,4 二唑 2 ,再通过芳胺的取代反应 ,得到目标化合物 2 取代氨基 5 吡唑基 1,3,4 二唑 3。2和 3的结构经1HNMR和元素分析验证 ;从质谱的碎片峰解析了 2A、2B 2个异构体的可能裂解途径。对中间体及目标化合物的杀菌活性测试表明 ,在质量分数为 0 0 0 5 %浓度下化合物 2A及 2B对芦笋茎枯菌的抑制率分别为 4 0 %和6 0 % ,3A 5和 3B 1也具有一定的杀菌活性。更多还原

【Abstract】 Methylthio-5-pyrazolyl-1,3,4-oxadizole 1 was oxidized by KMnO 4/HAc to give 2-methylsulfonyl-5-pyrazolyl-1,3,4-oxadiazole 2. Nucleophilic reaction of 2 with arylamines afforded the title compounds 2-arylamino-5-pyrazolyl-1,3,4-oxadiazoles 3. Structures of 2 and 3 were determined by elemental analysis, 1H NMR and mass spectrometry. The MS fragmentation patterns of compounds 2A and 2B were discussed. Bioassay showed that at a mass fraction of 0.005%, 2A and 2B inhibited Phoma asparagi by 40% and 60%. Compound 3A-5 and 3B-1 also have certain fungicidal activity.更多还原