Cu(I)‐Ming‐phos Catalyzed Enantioselective [3+2] Cycloadditions of Glycine ketimines to β‐Trifluoromethyl Enones

A catalytic asymmetric [3+2] cycloaddition of glycine ketimines with β‐CF3 β,β‐disubstituted enones was realized in the presence of a chiral copper(I)/Ming‐Phos complex. This method provides an access to construct highly functionalized pyrrolidines bearing three contiguous stereocenters, which including a trifluoromethylated all‐carbon quaternary stereocenter. The features of this reaction include high chemo‐, diastereo‐, enantioselectivity (up to >20:1 cr, >20:1 dr, 98% ee), readily available starting materials, well functional‐group tolerance and mild reaction conditions. Control experiments demonstrate that the fluoro‐substituent is crucial for the reactivity.