Chiral donor–acceptor azetines as powerful reactants for synthesis of amino acid derivatives

Abstract

Chiral 3-azetidinones are structural analogues of medicinally relevant β-lactams, however their synthesis and reactivity are underexplored. Here, the authors show a highly enantioselective copper-catalyzed [3 + 1]-cycloaddition generating 2-azetidines, which react with nucleophiles yielding amino acids via 3-azetidinones.