Sulfur-directed palladium-catalyzed C(sp3)–H α-arylation of 3-pyrrolines: easy access to diverse polysubstituted pyrrolidines

Abstract

A sulfur-directed palladium-catalyzed C(sp³)–H α-arylation of 3-pyrrolines has been disclosed by installing a thioacyl group as the directing group. The arylation reactions using arylboronic acids as coupling partners provided a variety of 2-aryl-3-pyrolines in moderate to good yields. Moreover, the α-arylated products were readily converted to various synthetically useful 3-pyrroline and pyrrolidine derivatives, especially polysubstituted pyrrolidines.