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Propylphosphonic Anhydride (T3P®) as Coupling Reagent for Solid-Phase Peptide Synthesis

Lookup NU author(s): Dr Othman AlmusaimiORCiD

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Abstract

Amidation is the predominant reaction within the pharmaceutical setting, and it is attracting greater attention due to the increased demand for therapeutic peptides. The high therapeutic efficacy and safety profile of peptides have placed these molecules in prime position within the pharmaceutical arena, which is reflected by these molecules receiving several approvals from various regulatory agencies each year. In this context, the demand for developing efficient strategies for peptide synthesis has also risen. Although propylphosphonic anhydride (T3P®), which has been recently proposed as a green coupling reagent, has shown good performance in solution, it has never been applied to solid-phase peptide synthesis (SPPS). Here we test the use of T3P® for SPPS. Satisfactory yields were achieved with a mild activation protocol. Various green solvents were tested and proved to be compatible with this coupling reagent. Several commonly used reagents cause allergic reactions or are susceptible to explosion under certain conditions. To overcome these issues, we propose T3P® as a potential alternative coupling reagent in SPPS.


Publication metadata

Author(s): Al Musaimi O, Wisdom R, Talbiersky P, de la Torre BG, Albericio F

Publication type: Article

Publication status: Published

Journal: ChemistrySelect

Year: 2021

Volume: 6

Issue: 11

Pages: 2649-2657

Print publication date: 19/03/2021

Online publication date: 16/02/2021

Acceptance date: 09/02/2021

ISSN (electronic): 2365-6549

Publisher: Wiley-VCH Verlag GmbH & Co. KGaA

URL: https://doi.org/10.1002/slct.202100123

DOI: 10.1002/slct.202100123


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