Abstract:
A metal-free facile and efficient two-step synthetic protocol for the preparation of 1, 4-benzoxazepine-5(2H)-ones derivatives has been developed. The protocol involves Ugi reaction followed by K2CO3 mediated highly regioselective 7-exo-dig intramolecular cyclization of less-nucleophilic oxygen with the pendant alkyne moiety of Ugi-propargyl precursor to afford the 1, 4-benzoxazepine-5(2H)-one derivatives in good to excellent yields.