新型二芳基吡唑衍生物的合成及其抑菌活性

Synthesis of Novel Diarylpyrazole Derivatives and Their Fungicide Activity

水杨醛与2,4-二氯苯乙酮缩合形成α,β不饱和酮后与水合肼关环形成3-(2,4-二氯苯基)-5-(2-羟基苯基)吡唑(2),2与烷基酰氯反应合成了6个未见文献报道的3-(2,4-二氯苯基)-5-(2-酯基苯基)-4,5-二氢-N-酰基吡唑衍生物(3a～3f),其结构经1HNMR,IR和元素分析表征。对3进行了初步生物活性测试,结果表明3浓度为50mg·L-1时,3f,3d对水稻纹枯菌的抑菌率分别为77.4%,60.3%,对稻瘟病菌的抑菌率分别为66.3%,69.2%;3e对油菜菌核菌抑菌率为79.2%。

（E） -1 - （ 2,4-dichlorophenyl） -3- （ 2-hydroxyphenyl ） prop-2-en-1 -one （2） was prepared by the reaction of 1-（2,4-dichlorophenyl） ethanone and salicylaldehyde and then cyclization with hydrazine monohydrate. Six novel 2- [ 1-acetyl-3- （2,4-dichlorophenyl） -4,5-dihydro-1H-pyrazol-5-yl ] pheny lacetate derivatives（3a-3f） were synthesized from 2 and acyl chloride. The structures were characterized by ^1H NMR, IR and elemental analysis. The biological activity experimental results showed that inhibition rate of 3f, 3d at 50 mg·L^-1 towards H. Oryzae were 77.4%, 60.3% and towards P. oryzae were 66.3%, 69.2%, respectively. Inhibition rate of 3e at 50 mg·L^-1 towards S. Sclerotiorum was 79.2%.