American Chemical Society
ol8b00992_si_001.pdf (1.76 MB)

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

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journal contribution
posted on 2018-04-17, 14:58 authored by Jun Pan, Xinyao Li, Xu Qiu, Xiao Luo, Ning Jiao
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.