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A nickel-catalyzed acetamidation and lactamization of arylboronic acids via a one-pot reaction with ynamides and N-hydroxyphthalimide is described. This protocol features with mild reaction conditions and a broad substrate scope, and has been successfully applied to late-stage functionalization of pharmaceuticals. Moreover, control reactions were conducted to elucidate a plausible mechanism.

Graphical abstract: Nickel-catalyzed acetamidation and lactamization of arylboronic acids

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