2-甲基-5-氰基-嘧啶-4-基-芳酰胺的合成与生物活性

Synthesis and Biological Activity of Aromatic Amide Derivatives Containing 2-Methyl-pyrimidine-5-carbonitrile Moiety

[目的]寻找高活性的嘧啶酰胺类化合物。[方法]以氰基乙酰胺为原料,通过缩合、环化、缩合等步骤合成了7个2-甲基-5-氰基-嘧啶苯甲酰胺化合物,并对目标化合物进行生物测试。[结果] 7个目标化合物通过1H NMR,13C NMR,MS和元素分析进行确证其结构。生物活性测试标明:化合物质量浓度在50 mg/L时,化合物4c对油菜菌核病菌(Sclerotinia sclerotiorum)、马铃薯晚疫病菌(Phytophthora infestans)、水稻纹枯病(Thanatephorus cucumeris)、小麦赤霉病菌(Gibberella zeae)具有中等抑制率;同时化合物4f在200 mg/L时对玉米螟虫(Pyrausta nubilalis)具有100%的致死率。[结论] 2-甲基-5-氰基-嘧啶芳甲酰胺化合物具有较好的生物活性,在其结构上进一步修饰,期望得到活性较高的化合物。

[Aims]This study aims to search for pyrimidine amide with high biological activities.[Methods]Seven aromatic amide derivatives containing 2-methyl-pyrimidine-5-carbonitrile moiety were synthesized through three step reactions including condensation,cyclization and condensation.And their insecticidal activities and fungicidal activities were evaluated.[Results]The structures of title compounds were characterized by 1H NMR,13C NMR,MS and elemental analysis.The results of biological bioassay showed that the compound 4c had moderate inhibitory activities against Sclerotinia sclerotiorum,Phytophthora infestans,Thanatephorus cucumeris and Gibberella zeae at the concerntration of 50 mg/L.were similar to that of azoxystrobin.Compound 4 f showed 100%mortality against Pyrausta nubilalis at 200 mg/L.[Conclusions]Aromatic amide containing 2-methyl-pyrimidine-5-carbonitrile moiety exhibited good biological activities and the structural modification based on aromatic amide containing 2-methyl-pyrimidine-5-carbonitrile moiety might be obtained with good biological activities.