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.