Asymmetric Construction of Functionalized Cyclopenta[b]pyrrolines via Cascade Aza-Piancatelli/Hydroamination Reactions

A chiral Brønsted acid/Pd that cooperatively catalyzed the asymmetric cascade aza-Piancatelli rearrangement/hydroamination of readily accessible alkynyl-functionalized tertiary furylcarbinols with anilines has been developed. This protocol provides expedient access to a variety of densely functionalized cyclopenta[b]pyrroline derivatives in high yields with excellent enantioselectivities.