摘要/Abstract

设计了1，2，4-三唑苯甲酰胺衍生物的合成路线，该路线包括2，6-二氯苯腈与1，2，4-三唑的催化偶联、腈的酰胺化、酰胺重氮化水解及酸的酰胺化等步骤.采用该路线合成了14个未见文献报道的1，2，4-三唑苯甲酰胺衍生物，其结构用¹H NMR、¹³C NMR和HRMS进行了表征；利用平皿法测试了它们对小麦全蚀病和小麦根腐病病原菌的抑制活性.结果表明，化合物2-氯-N-苯基-6-（1H-1，2，4-三唑-1基）苯甲酰胺（7i）在100 mg/L浓度下对供试小麦全蚀病病原菌抑制率达到80%，在50和25 mg/L的浓度下抑制率接近对照硅噻菌胺的水平，而对能引起小麦根腐病的假禾谷镰刀菌的抑制活性不显著.
关键词: 1,2,4-三唑苯甲酰胺衍生物, 合成, 小麦全蚀病病原菌, 抑菌活性
The synthetic route of substituted 1,2,4-triazole benzamide derivatives was explored, which included several steps such as catalytic cross-coupling of 2,6-dichlorobenzonitrile with a triazole, amidation of nitrile, diazotization of amide and hydrolysis, and amidation of acid. Unreported 14 new 1,2,4-triazole benzamide derivatives were synthesized. Their chemical structures were characterized by ¹H NMR, ¹³C NMR and HRMS. Their antifungal activities against Gaeumannomyces graminis var. tritici and Fusarium pseudocerealum were evaluated in vitro by the plate method. The results indicated that antifungal activities of compound 2-chloro-N-phenyl-6-(1H-1,2,4-triazol-1-yl)benzamide (7i) against Gaeumannomyces graminis var. tritici reached up to 80% at the concentrations of 100 mg/L, and were comparable to the control level of silthiopham at the concentrations of 50 and 25 mg/L. However, these compounds didn't show obvious antifungal activities against Fusarium pseudocerealum.
Key words: 1,2,4-triazobenzamide derivatives, synthesis, Gaeumannomyces graminis var. tritici, antifungal activity


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