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Updated: Sep 13, 2025

Split-and-pool Synthesis and Characterization of Peptide Tertiary Amide Library
Published on: June 20, 2014
Base-promoted dynamic amide exchange: efficient access to isotopically enriched tertiary amides
Quentin Lemesre1, Rémi Blieck1, Antoine Sallustrau1
1Service de Chimie Bio-organique et Marquage, CEA, DMTS, Université Paris-Saclay Gif-sur-Yvette F-91191 France davide.audisio@cea.fr.
Abstract:
Amide isotope labeling is a crucial tool in drug discovery and development. However, current methods label the desired peptide bond in a multi-step fashion. This study presents novel strategies for amide isotope exchange through transamidation and amide metathesis. By optimizing reaction conditions and exploring substrate scope, we achieved direct labeling of both amine and carbonyl moieties. These findings pave the way for more sustainable isotope labeling technologies. Furthermore, preliminary examples of isotope-containing waste recycling demonstrate a crucial step towards a greener future for isotope chemistry.
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