为了寻求以天然产物为先导结构的绿色、高效新型杀菌剂,以苯甲腈、3-溴丙酮酸乙酯和不同取代苯胺为原料,通过活性亚结构拼接合成了 12 个 N-(苯基)噻唑酰胺类衍生物(6a～6l).产物结构均经过1 H NMR、13 C NMR和HR-MS(MSI)表征.杀菌活性结果显示:该类化合物对水稻纹枯病菌、白芨白绢病菌和水稻稻瘟病菌有良好的抑制作用.化合物6c和6l对水稻稻瘟病菌的EC50值分别为0.015 mmol/L和0.020 mmol/L,优于对照药剂申嗪霉素(EC50 =0.031 mmol/L),其作为以天然产物为先导结构的新型杀菌剂,值得进一步探索研究.
Synthesis and Fungicidal Activity of The N-(Phenyl)Thiazolamide Derivatives
Seeking green,high-efficiency new fungicides with natural products as the leading struc-ture.Using benzonitrile,ethyl 3-bromopyruvate,and different substituted anilines as raw materials,a series of twelve N-(phenyl)thiazole amide derivatives(6a～6l)were synthesized by splicing active substructures.And confirmed by 1 H NMR,13 C NMR,and HR-MS(MSI)analysis.The results of fun-gicidal activity showed that the compounds had remarkable antifungal activity on R.solani,S.rolfii.and M.oryzae,and the EC50 values of compounds 6c and 6l against M oryzae were 0.015 mmol/L and 0.020 mmol/L better than the commercial fungicide phenazine-1-carboxylic acid(EC50 = 0.031 mmol/L).Compounds 6c and 6l can be used as a new fungicide with natural products as the lead structure and deserves further exploration.
thiazoleamidesynthesisfungicidal activityThiasporine A
万方数据
维普
