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

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 MeSiN 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.