Boc-α-methyl-D-phenylalanine is employed in peptide synthesis as a Boc-protected amino acid derivative, where the tert-butoxycarbonyl (Boc) group safeguards the amino function to enable selective reactions during peptide bond formation. It is especially useful in creating modified peptides and peptidomimetics, with the α-methyl substituent providing steric hindrance that modifies peptide conformation and improves stability. In medicinal chemistry, it facilitates the design of enzyme inhibitors and receptor ligands by exploiting its chiral center for targeted biological activity. Furthermore, it acts as a key building block in pharmaceutical development for treatments addressing neurological disorders and metabolic diseases.