The β-lactam antibiotics are among the most commonly prescribed drugs in the world and their importance has been demonstrated by the isolation and syntheses of several classes of these agents. Of the synthetic routes used to access this interesting scaffold, the Kinugasa reaction utilizes a convergent strategy based on cycloaddition between readily available terminal alkynes and nitrones. Asymmetric versions involving chiral catalysts, chiral auxiliaries or chiral substrates have also been reported. Intramolecular Kinugasa reactions are also developed. -turn based pharmacophore design became easy with the synthesis of peptidyl -lactam by this reaction. This article gives a brief overview of the Kinugasa reaction and of recent advances since its discovery