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Chiral ε-sultams, with their unique strain cyclic structure, are a type of molecule with important biological activities. A facile enantioselective aza-Friedel–Crafts reaction of seven-membered cyclic N-sulfonylimines with naphthols was developed with a cinchona alkaloid-based bifunctional organocatalyst, giving chiral ε-sultams with an enantiomeric excess of up to 92%.

Graphical abstract: Facile synthesis of chiral ε-sultams via an organocatalytic aza-Friedel–Crafts reaction

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