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A rhodium(III)-catalyzed intramolecular oxidative annulation of O -substituted N -hydroxyacrylamides for the construction of indolizinones via sequential C(sp 2 )-H activation and C(sp 3 )-H amination has been developed. This approach shows excellent functional-group tolerance. The synthesized scaffold forms the core of many natural products with pharmacological relevance.

Intramolecular cascade annulation triggered by rhodium(III)-catalyzed sequential C(sp2)–H activation and C(sp3)–H amination

Intramolecular cascade annulation triggered by rhodium(III)-catalyzed sequential C(sp²)–H activation and C(sp³)–H amination