Copper-catalyzed [3+2] annulation of O -acyl ketoximes with 2-aryl malonates for the synthesis of 3-aryl-4-pyrrolin-2-ones.

A copper-catalyzed [3+2] annulation of O -acyl ketoximes with 2-aryl malonates for the concise synthesis of 3-aryl-4-pyrrolin-2-ones has been developed. The advantage of this method lies in the use of O -acyl oximes as an internal oxidant to generate the nucleophilic enamines and electrophilic p -quinone methides concurrently. The subsequent nucleophilic addition undergoes selectively on the α-C of malonates.