β-Methyl-branched α-amino acids are important motifs in peptide therapeutics. However, only few methods on their synthesis have been reported to date. Herein we report an efficient, one-step synthesis of these β-Me-branched α-amino acids through the deoxygenative arylation of threonine, yielding a diverse scope of noncanonical α-amino acids with good functional group tolerance. Our method could also be extended to the deoxygenative arylation of 3-hydroxyproline, giving access to various therapeutically relevant arylated amino acids.
Stouwie et al. (Mon,) studied this question.