Direct Asymmetric Formal [3 + 2] Cycloaddition Reaction of Isocyanoesters with β‑Trifluoromethyl <i>β,β</i>-Disubstituted Enones Leading to Optically Active Dihydropyrroles

A highly enantioselective copper-catalyzed [3 + 2] cycloaddition reaction of <i>α-</i>isocyanoesters with <i>β,β</i>-disubstituted enones has been developed. Dihydropyrroles were obtained in excellent yields and enantioselectivity by employing an inexpensive copper catalyst. This process provides a scalable and efficient route for the synthesis of highly enantioselective 2,3-dihydropyrroles bearing a trifluoromethylated all-carbon quaternary stereocenter. The salient feautures of this reaction include high efficiency, operational simplicity, high diastereoselectivity and enantioselectivity, a broad substrate scope, outstanding functional group tolerance, and products exhibiting high utility for further transformations