新型5-芳基吡唑衍生物的合成与抑菌活性

以2-氯苯甲醛与酮缩合形成α,β不饱和酮,与水合肼关环形成5-(2-氯苯基)吡唑结构骨架,合成了18种未见文献报道的5-(2-氯苯基)-3-甲基(或乙基)-4,5-二氢-N-酰基吡唑类衍生物,并经过元素分析、红外光谱、核磁共振氢谱测试技术对其结构进行了表征。对新合成的化合物进行了初步生物活性测试。结果表明,化合物3ae对稻瘟病菌的抑菌率达到60.2%,化合物3bf对油菜菌核菌的抑菌率达到56.7%。化合物3aj和3bj对供试病菌均有50%左右的抑菌率。

Synthesis and Fungicidal Activity of Novel 5-Arylpyrazole Derivatives

4-(2-Chlorophenyl)but-3-en-2-one was prepared via the condensation of 2-chlorobenzaldehyde and acetone followed by cyclization with hydrazine monohydrate. Eighteen new 5-(2-hydroxyphenyl)-3-methyl(or ethyl)-4,5-dihydro-N-acylpyrazole derivatives were synthesized and characterized by elemental analysis, IR and 1H NMR. The experimental results show the inhibition rate of compound 3ae against P.oryzae was up to 60.2%, the inhibition rate of compound 3bf against S.Sclerotiorum was up to 56.7%. Conpounds 3aj and 3bj exhibited certain fungicidal activity against H.Oryzae, P.oryza, S.Sclerotiorum, with inhibition rate of up to 50%.