中文摘要：

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.

英文摘要：

1,2,3-Triazole amide derivatives containing triazole as a bioisoster of pyrazole were designed according to ＂bioisoteric replacement＂ from pyrazole amide fungicide.Seventeen novel 1-substituted-1H-1,2,3-triazole-4-carboxamide derivatives were quickly synthesized through the copper（I）-catalyzed Huisgen 1,3-dipolar cycloadditions of organic azide compounds and propiolamide,which was synthesized from propiolic acid.With Cu/C as the catalyst and triethylamine as the additive,the coupling product substituted bis-1,2,3-triazole 17 was obtained in a moderate yield when cyclizing intermediate N-（3,4-dimethoxy-phenethyl）propiolamide（4a） and 2-azido-1,1,1-trifluoroethane（14）.The structures of the target compounds were confirmed by 1H NMR spectra,elemental analysis or high resolution mass spectra（HRMS）.The investigation of the target compound bioactivities show that,some of them like 6a,6e,6k and 6l perform good herbicidal activity at 100 μg/mL,even though they have a poor fungicidal action.