Natural SciencesChemistryMedicinal ChemistryCatalysisOrganic ChemistrySynthetic Medicinal ChemistryOrganic SynthesisOxidation ReactionsRedox ProcessesBioactive Plant CompoundsCopper-catalyzed CouplingCopper-catalyzed OxidationLabelingOxazole ChemistryOxazole SynthesisOxidative CouplingOxidative Cross-coupling
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.
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