Abstract A selective synthetic method of the 2, 5-biaryltriazolones has been developed via copper-catalyzed N-arylation reaction. Aryltriazolones, which were readily prepared from commercially available compounds, were N-arylated to 2, 5-biaryltriazolones with high regioselectivity. This approach allows for access to a variety of 2, 5-biaryl-1, 2, 4-trizol-3- ones in a simple and practical manner.