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为了寻找具有较高除草活性的农药先导化合物,将吡唑环与双酰肼结构进行拼接,设计合成了13个未见报道的含吡唑环的双酰肼类目标化合物6a~6m,其结构均通过核磁共振氢谱及高分辨质谱确认。培养皿法测定结果表明:在200 mg/L下,化合物N'-(2-(2,4-二氯苯氧基)乙酰基)-3-(二氟甲基)-1-甲基-1H-吡唑-4-甲酰肼(6i)对小麦Triticum aestivum、油菜Brassica campestris、高粱Sorghum bicolor、萝卜Raphanus sativus和黄瓜Cucumis sativus根、茎的抑制率均达80%以上。盆栽试验表明:在有效成分150 g/hm2剂量下,采用苗后茎叶喷雾处理,化合物6i对反枝苋Amaranthus retroflexus和鳢肠Eclipta prostrata的抑制率均达80%;相同剂量下采用苗前土壤喷雾处理,6i对反枝苋A.retroflexus的抑制率也达80%。
In order to find a pesticide lead compound with high herbicidal activity, pyrazole ring and bis-hydrazide structure were spliced together to design and synthesize 13 unidentified bis-hydrazide target compounds 6a ~ 6m. The structure of All were confirmed by 1H NMR and HRMS. The results of the petri dish assay showed that at 200 mg / L, the compound N '- (2- (2,4-dichlorophenoxy) acetyl) -3- (difluoromethyl) The inhibitory rates of 1H-pyrazole-4-carboxylic acid hydrazide (6i) on roots and stems of wheat Triticum aestivum, Brassica campestris, sorghum bicolor, Raphanus sativus and cucumber Cucumis sativus were more than 80%. Pot experiments showed that the compound 6i inhibited the growth of Amaranthus retroflexus and Eclipta prostrata by 80% at the dose of 150 g / hm2 of the active ingredient. With the same dose, Spray treatment, 6i on Amaranthus retrovirus A.retroflexus inhibition rate of up to 80%.