Recent Developments on Solid-Phase Peptide Synthesis in a Green Context
Fernando Albericio
Research Professor, Universitiy of KwaZulu-Natal
The entry of large and complex peptide-based drugs into the market has been possible thanks to a simple discovery, namely solid-phase synthesis. During these days, we are celebrating the 60th anniversary of the first formal publication of the Solid-Phase Peptide Synthesis (SPPS) technique by the Nobel Laureate R. Bruce Merrifield. Since then, the initial SPPS concept has enormously evolved. Lastly, the field is challenged to be more sustainable, using fewer hazardous solvents and reagents.
During this presentation, we will review our last work focused on reducing the consumption of solvents. Furthermore, we will introduce some new green solvents to be used in SPPS, coupling reagents, and additives.
Finally, we will discuss a new category of protecting groups that are stable under all the synthetic conditions, such as basic or acidic, and, after a manipulation, they are removed at the end of the synthetic process by common reagents. This step can be performed when the peptide is still anchored to the resin, or once the peptide is in solution. These new concepts of protecting groups based on the Safety-Catch concept facilitate the synthesis and manipulation of complex peptides.
Fernando Albericio is Research Professor at the University of KwaZulu-Natal (South Africa), and Emeritus Professor of Organic Chemistry at the University of Barcelona (Spain)
His major research interests cover practically all aspects of peptide synthetic methodology as well as synthesis of peptides and small molecules with therapeutic activities (cancer and infectious diseases). Lastly, he was working in greening the solid-phase peptide synthesis processes. He has published more than 1000 scientific articles graduated more than 75 Ph.D. students.