Alkynyliodonium Salt Mediated Alkynylation of Azlactones: Fast Access to Cα-Tetrasubstituted α-Amino Acid Derivatives

An efficient electrophilic alkynylation of azlactones (oxazol-5(4H)-ones) is developed using alkynyl(phenyl)iodonium salts as the electrophilic alkyne source. After remarkably short reaction times, the desired alkyne functionalized azlactones are obtained in 60-97% yield and can be transformed easily into a variety of quaternary alpha-amino acid derivatives.