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An efficient and concise catalyst-free one-pot synthetic protocol for obtaining dihydroisoquinoline derivatives has been developed via the three-component condensation of isoquinolines with β-keto acids and sulfonyl chlorides. This transformation involving decarboxylative dearomatization worked well under mild and water-mediated conditions. The protocol tolerates diverse functional groups, furnishing the dihydroisoquinoline products in good to excellent yields.

Graphical abstract: The catalyst-free decarboxylative dearomatization of isoquinolines with β-keto acids and sulfonyl chlorides in water: access to dihydroisoquinoline derivatives

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