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Green Transformation of Solid-Phase Peptide Synthesis

Abstract:

Peptides play key roles in medicinal chemistry, being found in therapeutics and diagnostic agents, among others. Furthermore, their synthetic protocols have also been optimized for other fields such as the solid-phase organic synthesis of other organic compounds. However, the classical protocols for peptide synthesis fall short of Green Chemistry parameters. The excess of reagents and solvents used in classical protocols is costly. Moreover, the widely used hazardous chemicals pose a threat to the environment and to human health. In this review, we examine peptide synthesis in the context of green chemistry and address its pros and cons. Furthermore, we discuss several attempts to make peptide synthesis greener. These attempts have followed two major pathways, namely reducing the amount of material used or replacing hazardous materials for friendlier ones. Although this work focuses mostly on the solid-phase peptide synthesis approach, a brief description of some reagents, solvents, methods or strategies used in solution is given because these compounds could be easily adapted to the solid-phase mode.