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-cyclohexylidenehydantoin and their derivatives

作　　者：雷建平[1] 董宏波[1] 徐志红[1] 汤博[1] 王明安[1] 

机构地区：[1]中国农业大学应用化学系,北京100193

出　　处：《农药学学报》2012年第4期445-448,共4页Chinese Journal of Pesticide Science

基　　金："十二五"国家科技支撑计划项目(2011BAE06B04);国家自然科学基金资助项目(21172254)

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50μg/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8.48μg/mL。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.

关 键 词：5-亚环己基-(2-硫代)-咪唑-2 4-二酮 合成 杀菌活性 

分 类 号：O626.23[理学—有机化学] S482.2[理学—化学]