Despite the tremendous progress in transition metal-catalyzed synthetic strategies for valuable organic compounds, there are strong unmet demands for the development of sustainable synthetic methods in response to the problems of pollution and energy shortage facing our society. Accordingly, step- and atom-economical approaches for the synthesis of useful compounds have emerged as a dominant theme in organic synthesis.<br/>In terms of atom-economy, rearrangement is the one of the most efficient synthetic strategy that can convert “easy-to-prepare” precursors into the “difficult-to-make” products. We disclosed a simple transition metal-free strategy involving Smiles rearrangement to synthesize pyrido[1,2-a]indolone derivatives. This reaction features environmentally friendly reaction conditions, a high atom- and cost-economy, a short reaction time, and a broad range of substrate scope with high reaction efficiency.

Application of the smiles rearrangement: Transition metal-free synthesis of pyridoindolones

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