The invention relates to an N2-substituted 1,2,3-triazole derivative for a Cu (I) ligand as well as a preparation method and an application of the N2-substituted 1,2,3-triazole derivative. The derivative has the structural general formula as shown in the specification, wherein R is alkyl or aryl, R' is H atom, alkyl or aryl, and X is CH or N atom. The preparation method comprises the following steps: mixing NH-1,2,3-triazole, halogenated hydrocarbon and K2CO3, stirring, reacting, extracting and drying after the reaction is ended, and filtering and concentrating to obtain a coarse product; separating and purifying through thin-layer column chromatography on silica gel, thus obtaining the product; or mixing NH-1,2,3-triazole, halogenated aromatic hydrocarbon, CuX and K2CO3, by taking DMF as a solvent, heating, reacting, extracting and drying after the reaction is ended, filtering and concentrating to obtain a coarse product, separating and purifying through thin-layer column chromatography on silica gel, thus obtaining the product. The invention has the advantages that the N2-substituted 1,2,3-triazole derivative is simple in synthesis and stable in property and has the characteristics of small catalyst amount, mild reaction conditions, high product yield and high substrate adaptability.