(4-亚甲基-5-羰基-3-四氢呋喃基)-苯甲酸甲酯衍生物的合成及其杀菌活性

    Synthesis and fungicidal activity of (4-methylene-5-oxo-tetrahydrofuran-3-yl) methyl benzoate derivatives

    • 摘要: 为了探索天然产物Cedarmycins衍生物的结构与活性关系,以α-亚甲基-β-羟甲基-γ-丁内酯为起始原料,经过与不同取代的羧酸缩合,合成了19个新的(4-亚甲基-5-羰基-3-四氢呋喃基)-苯甲酸甲酯衍生物。杀菌活性测定结果表明,该类衍生物具有广谱的杀菌活性,尤其对水稻纹枯病菌Rhizoctonia solani和辣椒疫霉Phytophthora capsici显示出很强的杀菌活性,其中化合物2e(R=2,4-2Cl)对这2种病菌的EC50值约为1.6 mg/L。

       

      Abstract: In order to elucidate structure-activity relationship of natural product Cedarmycins,a series of novel (4-methylene-5-oxo-tetrahydrofuran-3-yl) methyl benzoate derivatives (2a-2s) were synthesized by condensation of 4-(hydroxymethyl)-5-methylene-dihydrofuran-2(3H)-one with various substituted benzoate acids.The preliminary bioassay showed that some of these compounds have good fungicidal activity,especially against Rhizoctonia solani and Phytophthora capsici.The EC50 value of compound 2e (R=2,4-2Cl) were about 1.6 mg/L for the above fungus.

       

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