Facile access to versatile aza-macrolides through iridium-catalysed cascade allyl-amination/macrolactonization

Abstract

Direct access to benzo-fused aza-macrolides was successfully achieved through iridium-catalysed intermolecular decarboxylative coupling of vinylethylene carbonates with isatoic anhydrides under relatively mild reaction conditions. Notably, this reaction proceeded through sequential allyl-amination/macrolactonization upon extrusion of CO₂. Moreover, favourable fluorescence properties could be observed in the title macrocyclic products.