Cu(I)-Catalyzed C(sp3)–H Functionalization of Amino Acids with Benzimidate and Reactive Oxygen Species (ROS) To Synthesize Triazines and 2-Pyrrolidinones

An easily accessible Cu(I)-catalyzed regioselective oxidative C–N/C–O cross-coupling organic transformation has been disclosed for the syntheses of variably functionalized triazines and N-benzoylpyrrolidin-2-ones through the involvement of C(sp³)–H bond functionalization, which is unknown in the literature. This general synthetic method is extended for decarboxylative oxidation of amino acids to install carbonyl functionality. It facilitates the formation of 2–3 new bonds through the cross-coupling strategy involving benzimidates, amino acids, and in situ-generated reactive oxygen species (ROS) from the aerial O₂ as the sole oxidant. The key utilities of the new reactions are demonstrated by its operational simplicity, regioselectivity, robustness, and broad substrate scope with high yields.