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以吡唑酰胺类杀菌剂为模板,应用“生物等排原理”设计了1,2,3-三唑甲酰胺类具有等排结构的化合物,从丙炔酸出发合成丙炔酰胺后,利用Cu(I)催化的1,3-偶极环加成反应,使其与叠氮化合物反应,快速合成了17个结构新颖的1-取代-1H-1,2,3-三唑-4-甲酰胺类化合物.当使用Cu/C催化时,中间体N-(3,4-二甲氧基苯基乙基)丙炔酰胺(4a)与2,2,2-三氟乙基叠氮(14)在三乙胺作添加剂的条件下,可以获得中等收率的偶联的1,2,3-三唑化合物17.所有目标化合物都通过核磁共振氢谱,元素分析或高分辨质谱的确认,并测试了其生物活性.结果表明,该类化合物虽无明显的杀菌活性,但在100μg/mL测试浓度下,化合物6a,6e,6k和6l均表现出较好的除草活性.
The pyrazole amide fungicides as a template, the application of “bioisosterism principle” designed 1,2,3-triazole formamide compounds with isosteal structure, starting from the synthesis of propiolic acid propiolic acid amide, The 1,3-dipolar cycloaddition catalyzed by Cu (I) was reacted with azide to synthesize 17 novel 1-substituted-1H-1,2,3-triazol-4 - carboxamides The intermediate N- (3,4-dimethoxyphenylethyl) propylamide (4a), when catalyzed with Cu / C, is reacted with 2,2,2-trifluoroethyl Nitrogen (14) Intermediate 1,2,3-triazole compounds 17 can be obtained in moderate yields with triethylamine as an additive 17. All target compounds were characterized by 1H nuclear magnetic resonance, elemental analysis or high resolution mass spectrometry The results showed that the compounds 6a, 6e, 6k and 6l showed good herbicidal activities at the concentration of 100μg / mL.