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

Abstract

Abstract A catalytic asymmetric [3+2] cycloaddition of glycine ketimines with β ‐CF 3 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 &gt;20:1 cr, &gt;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. magnified image