One-pot synthesis of 5-oxopyrrolidine-2-carboxamides via a tandem Ugi 4CC/SN cyclization starting from Baylis–Hillman bromides

A one-pot base-mediated synthesis of 5-oxopyrrolidine-2-carboxamides was developed. The reaction of Baylis–Hillman bromides 1, primary amines 2, isocyanides 3 and arylglyoxals 4 produced the 5-oxopyrrolidine-2-carboxamides 6 in good yields via a tandem Ugi condensation and intramolecular substitution at room temperature in the presence of Cs2CO3.