Synthesis of α-Methylated Amino Acids for Buchwald-Hartwig Cross-Coupling

Abstract

α-Methylated amino acids are valuable components in peptide drugs due to their ability to protect
peptides from enzymatic degradation. The objective of this work was to demonstrate that an α
methylated amino acid, bearing an alkyl amine side chain, could undergo cross-coupling with an
aryl halide via Buchwald-Hartwig amination. Progress has been made toward the synthesis of these
amino acids from N-benzyloxycarbonyl-D-alanine.