1-甲基-3-二氟甲基吡唑酰胺类化合物的合成及抑菌活性

Study on synthesis and antifungal activity of 1-methyl-3-difluoromethyl pyrazolamide derivatives

以1-甲基-3-二氟甲基吡唑-4-甲酸为原料,经过1-甲基-3-二氟甲基吡唑-4-甲酰氯与相应的氨基苯并杂环类、芳胺类化合物反应,得到了14个未见文献报道的吡唑-4-甲酰胺类化合物(6a～6g、7a～7g),其结构均通过1H NMR、MS和IR表征。抑菌活性测试结果表明,在100 mg/L下,目标化合物对供试植物病原菌均有不同程度的抑制作用,其中7a～7g的抑菌活性较高,部分对苹果炭疽病菌的抑制率在90%以上。

Fourteen novel pyrazol-4-amide derivatives were synthesized from 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid by the reaction of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carbonyl chloride with various amines.The structures of these compounds were confirmed by 1H NMR,MS,and IR.Antifungal activity test indicated that all of the synthesized compounds（6a-6g,7a-7g） showed different inhibition on tested plant pathogenic fungi at the concentration of 100 mg/L.The compounds 7a-7g exhibited good antifungal activity,and the growth inhibition rate of compounds 7a,7d,7g against Glomerella cingulata was above 90%.