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An Ir(III)-catalyzed relay aryl C–H bond carbenoid insertion cascade of N-aryl-2-pyridinamines with diazo Meldrum's acid has been developed. This method provides an efficient approach to multifunctionalized 1,3-dihydroindol-2-ones with a broad range of functional group tolerance. Furthermore, this protocol could be applied for the concise synthesis of bioactive hematopoietic growth factor analogues.

Graphical abstract: An Ir(iii)-catalyzed aryl C–H bond carbenoid functionalization cascade: access to 1,3-dihydroindol-2-ones

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