5-亚环己基-咪唑-2,4-二酮及其衍生物的合成及杀菌活性

Synthesis and fungicidal activity of 5-cyclohexylidene- hydantoin and their derivatives

摘要: 以环己酮及其衍生物和2-硫代-咪唑-2,4-二酮及咪唑-2,4-二酮膦酸酯为起始原料,经Knoevenagel 缩合反应和Wittig-Horner反应合成了10个5-亚环己基-咪唑-2,4-二酮系列衍生物,其中7个为新化合物,其化学结构经1H NMR、IR和MS确证。初步生物活性测定结果表明:在50 μg/mL 下,部分目标化合物对油菜菌核病菌 Sclerotinia scleotiorum 显现出良好的抑制活性,其中 7I和7J 的EC50分别为8.06 和8.48 μg/mL。

Abstract: A series of new 5-cyclohexylidene-hydantoin and their derivatives 7A-7J were synthesized via Knoevenagel and Wittig-Horner reaction using substituted cyclohexanone,and 2-thiohydantoin and hydantoin phosphonate as starting material.Their structures were confirmed by 1H NMR,IR and MS data.The preliminary bioassay showed that some of the compounds have good fungicidal activity against Sclerotinia scleotiorum at the concentration of 50 μg/mL.The EC50 value of compound 7I and 7J against S.scleotiorum were 8.06 and 8.48 μg/mL,respectively.