Rhodium-catalyzed annulation of hydrazines with vinylene carbonate to synthesize unsubstituted 1-aminoindole derivatives

Herein, we describe rhodium-catalysed C-H bond activation for [3 + 2] annulation using hydrazide and vinylene carbonate, providing an efficient method for synthesising unsubstituted 1-aminoindole compounds. Characterised by high yields, mild reaction conditions, and no need for external oxidants, this transformation demonstrates excellent regioselectivity and a wide tolerance for various functional groups. The step-economical synthesis of C2, C3-unsubstituted 1-aminoindole derivatives through rhodium-catalyzed annulation of hydrazines with vinylene carbonate.