摘要/Abstract

为了寻找高杀菌活性的农药先导化合物, 设计合成了一系列未见文献报道的含三唑的烯丙基苯甲酸酯类化合物, 其结构经¹H NMR和HRMS进行了确证, 用X射线单晶衍射测定了(R,S)-(Z)-1,3-二苯基-2-(1H-1,2,4-三唑-1-基)烯丙基2,3-二氯苯甲酸酯(5j)的晶体结构. 生物活性测定结果表明, 在50 mg/L的浓度下, (R,S)-(Z)-1,3-二苯基-2-(1H-1,2,4-三唑-1-基)烯丙基苯甲酸酯(5a), (R,S)-(Z)-1,3-二苯基-2-(1H-1,2,4-三唑-1-基)烯丙基2-氟苯甲酸酯(5g)和(R,S)-(Z)-1,3-二苯基-2-(1H-1,2,4-三唑-1-基)烯丙基3-甲基苯甲酸酯(5n)对油菜菌核的抑菌率均达到了70%以上, 显示出了较高的杀菌活性.
关键词: 关键词 三唑类杀菌剂, 合成, 杀菌活性, 构效关系(SAR)
In order to find pesticide lead compounds with high fungicidal activity, a series of unreported allyl benzoate compounds containing triazole were designed and synthesized. The structures were confirmed by ¹H NMR and HRMS, and the crystal structure of (R,S)-(Z)-1,3-diphenyl-2-(1H-1,2,4-triazol-1-yl)allyl 2,3-dichlorobenzoate (5j) was determined by X-ray single crystal diffraction. The bioassay results showed that (R,S)-(Z)-1,3-diphenyl-2-(1H-1,2,4-triazol-1-yl)allyl benzoate (5a), (R,S)-(Z)-1,3-diphenyl-2-(1H-1,2,4-triazol-1-yl)allyl 2-fluorobenzoate (5g) and (R,S)-(Z)-1,3-diphenyl-2-(1H-1,2,4-triazol-1- yl)allyl 3-methylbenzoate (5n) exhibited good control efficacy against Sclerotinia sclerotiorummore than 70% at 50 mg/L.
Key words: triazole fungicide, synthesis, fungicidal activity, structure activity relationship (SAR)


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