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Advances in Fmoc solid‐phase peptide synthesis
Authors:Raymond Behrendt  Peter White  John Offer
Institution:1. Novabiochem, Merck & Cie, Schaffhausen, Switzerland;2. Novabiochem, Merck Chemicals Ltd, Beeston, UK;3. The Francis Crick Institute, London, NW1 2BE, UK
Abstract:Today, Fmoc SPPS is the method of choice for peptide synthesis. Very‐high‐quality Fmoc building blocks are available at low cost because of the economies of scale arising from current multiton production of therapeutic peptides by Fmoc SPPS. Many modified derivatives are commercially available as Fmoc building blocks, making synthetic access to a broad range of peptide derivatives straightforward. The number of synthetic peptides entering clinical trials has grown continuously over the last decade, and recent advances in the Fmoc SPPS technology are a response to the growing demand from medicinal chemistry and pharmacology. Improvements are being continually reported for peptide quality, synthesis time and novel synthetic targets. Topical peptide research has contributed to a continuous improvement and expansion of Fmoc SPPS applications. Copyright © 2015 European Peptide Society and John Wiley & Sons, Ltd.
Keywords:solid‐phase peptide synthesis  Fmoc/tBu  aspartimide  peptide thioester  post‐translational modification  protecting group  racemisation
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