Form,ation of dihydropyridone- and pyridone-based peptide analogs through aza-annulation of β-enamino ester and amide substrates with α-amido acrylate derivatives

摘要

The aza-annulation of β-enamino ester and amide substrates with the mixed anhydride of 2-acetamidoacrylic acid was used for the efficient construction of highly substituted α-acetamido δ-lactam products. With the α-acetamido substitutent, lactam functionality, and γ-carboxylate group, these δ-lactam products represent an interesting class of conformationally restricted dipeptide analogs. The framework of this lactam hub is structurally related to that of and α-anubi acid coupled with a β-anubi acud.