Synthetic Methodologies for the Preparation of Arginine-Proline Derivatives

Proline derivatives bearing arginine side chain elicit great interest both in medicinal and biological chemistry, due to the combination of unique proline conformational properties with the important role played by the arginine polar side chain in protein molecular recognition. This review focuses on synthetic methodologies to obtain 3- and 4-substituted arginine-proline derivatives, which are useful compounds both as building blocks in peptide syntheses, and as potential ligands of specific proteins.