Copper(I)‐Catalyzed Intramolecular Direct C‐Arylation of Azoles with Aryl Bromides

Abstract

Abstract A concise route to access 5 H ‐imidazo[2,1‐ a ]isoindole heterofused compounds by copper(I)‐catalyzed intramolecular coupling of non‐activated aryl bromides with azoles is reported. With CuI as catalyst, 1,10‐phenanthroline as ligand, and K 3 PO 4 as base, the reactions of 1‐(2‐bromobenzyl)‐1 H ‐imidazoles in DMF/ o ‐xylene (1:1, V : V ) at 145°C afford the corresponding substituted 5 H ‐imidazo[2,1‐ a ]isoindoles in high yields via intramolecular C‐arylation.