The synthesis of substituted 2-hydroxy-indolin-3-ones has attracted considerable attention of synthetic chemists because they present in numbers of natural products and biologically active molecules. Herein, a novel and convenient copper-catalyzed oxidative intramolecular cyclization of N-(2-acetylphenyl)picolinamide for the synthesis of 2-hydroxy-indolin-3-ones has been developed. Moreover, the detailed mechanism presented is supported by control experiments and density function-al theory calculations. This method provides direct access to 2-hydroxy-indolin-3-ones in high yield and good functional group tolerance. Atom-economy, avoidance of the preparation for substrates and step economy make this protocol be practical. This strategy provides an alternative synthetic method to ex-plore the synthetic application of various types of 2-hydroxy-indolin-3-ones and their enantiopure deriv-atives.