Abstract
A one‐pot synthesis of indole derivatives from readily available acetanilides and diazo compounds was developed. This IrIII‐catalyzed C–H alkylation and annulation reaction proceeds under mild conditions and generates molecular nitrogen and water as byproducts. Various types of synthetically versatile N‐substituted indoles, including N‐acetyl, N‐pivolyl, and N‐benzoyl indoles, were prepared.
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