Abstract
For many years, pharmaceutical companies have focused their attention on the development of drugs based on the biological activity of small molecules. More recently, peptides have been recognized as efficient active pharmaceutical ingredients. About 100 peptidic drugs have now reached the pharmaceutical market and many peptides are now in the pipeline of pharmaceutical companies. The building blocks that are used to make peptides are protected amino acids. Ball-milling technology has been applied to the preparation of these major biomolecules, producing an improvement over more classical methods (solution or solid-phase synthesis) since the amount of organic solvents – most of which are hazardous or detrimental to the environment – was greatly reduced. Progress made in the derivatization and protection of amino acids and peptide synthesis using ball-milling is reported in this chapter.