Used as a chiral building block in the synthesis of pharmaceuticals, particularly in the development of bioactive molecules and peptide mimetics. Its rigid diketopiperazine core provides structural stability and influences conformational preference, making it valuable in medicinal chemistry for designing enzyme inhibitors and receptor ligands. Commonly employed in asymmetric synthesis to introduce stereochemical control. Also found in research related to central nervous system agents due to the piperazine motif’s affinity for neurotransmitter receptors.