Tandem One-Pot Approach to Access 1,2,3-Triazole-fused Isoindolines through Cu-Catalyzed 1,6-Conjugate Addition of Me3SiN3 to p-Quinone Methides followed by Intramolecular Click Cycloaddition

Abstract

A Cu-catalyzed one-pot approach has been developed for the synthesis of 1,2,3-triazole-fused tricyclic heterocycles. This tandem approach actually involves the 1,6-conjugate addition of Me3SiN3 to o-alkynylated p-quinone methides followed by an intramolecular [3+2]-cycloaddition reaction. This protocol allowed us to access a wide range of 1,2,3-trazole-fused isoindoline derivatives in moderate to good yields.