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Asymmetric copper-catalysed intramolecular C–H insertion reactions of a series of α-diazo-β-keto sulfones are reported. Enantioselectivities of up to 82% ee were achieved in moderate to good yield. These results represent the highest level of enantiocontrol achieved to date for a copper-catalysed cyclopentanone synthesis via C–H insertion.

Graphical abstract: Asymmetric copper-catalysed intramolecular C–H insertion reactions of α-diazo-β-keto sulfones

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