Palladium‐Catalyzed Cascade Cyclization and Alkynylation of 2‐Alkynylphenols with Bromoalkynes

Abstract

A palladium‐catalyzed cascade synthesis of 3‐alkynylbenzofuran scaffolds has been developed through cyclization and alkynylation of 2‐alkynylphenols with bromoalkynes. A variety of 3‐alkynylbenzofuran derivatives were prepared in good yields under mild conditions. Notably, this protocol was applied to the late‐stage modification of bioactive molecule.