An facile, effective, copper-catalyzed one-pot approach to 2-benzyl-3,4-dihydroquinolin-1-ones has been successfully developed. The compounds were achieved by the reaction of tetrahydroisoquinoline, benzyl azide and benzaldehyde in one-pot fashion via nucleophilic addition reaction followed by oxidation. The desired products were afforded in the high yield of 50%～70%. Moreover, The effects of different catalyst, additives, reaction temperature and proportion of substrates on the reaction were also investigated. The results showed that the optimizing conditions of reaction were CuCl 2 as catalyst, CH 3 COOH as additive and toluene as solvent. A series of 2-benzyl-3, 4-dihydro-2H-isoquinolin-1-ones can be efficiently obtained under the optimizing conditions.