Copper-Catalyzed Oxygenation Approach to Oxazoles from Amines, Alkynes, and Molecular Oxygen

A novel and efficient oxygenation approach to trisubstituted oxazoles via a copper-catalyzed aerobic oxidative dehydrogenative annulation of amines, alkynes, and O₂ has been developed. This transformation combines dioxygen activation and oxidative C-H bond functionalization and provides a practical protocol for the preparation of oxazole derivatives, which are privileged units found in various bioactive compounds or other natural products. ¹⁸O-labeling experiments were conducted to reveal that oxygenation was involved in this chemistry.