含三唑结构的环己甲酰胺衍生物的合成及杀菌活性  

Synthesis and fungicidal activity of cyclohexanamide derivatives with triazole moeity

作　　者：杜琳 张斌 宁磊 王思敏 路慧哲[1] 张建军[1] 董燕红[1] DU Lin;ZHANG Bin;NING Lei;WANG Simin;LU Huizhe;ZHANG Jianjun;DONG Yanhong(College of Science,China Agricutural Universiy,Beijing 100193,China;Chinese Academy of Forestry Sciences,Beijing 100091,China)

机构地区：[1]中国农业大学理学院,北京100193 [2]中国林业科学研究院,北京100091

出　　处：《农药学学报》2020年第4期595-601,共7页Chinese Journal of Pesticide Science

基　　金：国家自然科学基金(31272075).

摘　　要：为寻找高效的杀菌活性化合物,在前期十三元氮杂大环内酯化合物Z13-5的基础上尝试进行结构改造,保留三唑与环己甲酰胺结构,通过酰胺化及叠氮-炔烃点击反应等设计并合成了26个未见文献报道的目标化合物,其结构均通过核磁共振氢谱(1H NMR)、碳谱(13C NMR)及高分辨质谱(HRMS)确证。初步杀菌活性测定结果表明:与化合物Z13-5相比,目标化合物的杀菌活性有所下降,在50 mg/L下,除化合物7g对辣椒疫霉病菌的抑制率可达91%外,其余化合物对供试病原真菌的抑制率均低于50%。In order to discover novel compounds with high fungicidal activities,a series of new compounds were designed using macrocyclic compound Z13-5 as the lead compound.And the triazole and cyclohexanamide moeities were retained.26 new target compounds were synthesized through azidation,azic-alkyne click reaction,etc,and characterized by 1H NMR,13C NMR and HRMS spectral data.Preliminary bioassay indicated that fungicidal activities of the target compounds were lower than compound Z13-5.At the concentration of 50 mg/L,the inhibition rates of most of the target compounds to the tested pathogenic fungi were less than 50%,except 7 g had 91%inbition rate to Phytophthora capsicum.

关 键 词：三唑 环己甲酰胺 酰胺化 点击反应 杀菌活性 

分 类 号：O626.26[理学—有机化学] TQ455.4[理学—化学]