Synthetic Studies of Thymosin Alpha-1 Fragments

Abstract

Background: According to F&S (Frost & Sullivan)’s annual report, there have been more than 40 marketed peptides worldwide till 2005. In the past three years, three new peptide drugs have been approved by the US Food and Drug Administration (Knut, 2005), which suggests that a new era of treatment by peptide drugs is coming. Today, the benefits of peptide drugs have been accepted by increasing numbers of people, and hundreds of peptides are in development. Aim: This research programme was designed to explore a suitable method for synthesis of the specific fragments of thymosin alpha-1 which were reported to have a potent anticancer activity. We were also interested in investigating new coupling reagents which would be more efficient, easily-operated, and economic in the liquid-phase. Methods: To achieve accurate results, a series of analytical techniques was used in this study. This included TLC, LC, NMR, IR, Melting point, MS, as well as evaporation, extraction, desiccation, filtration and distillation. Results: A new coupling reagent BEPB has been investigated that gives a better reaction yield in a much shorter time. It also has been proved by the synthesis of thymosin alpha-1 fragments in the liquid phase. No partial racemisation was observed.