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Lookup NU author(s): Thomas Carton, Dr Jessica Graham, Professor Mike WaringORCiD
This work is licensed under a Creative Commons Attribution 4.0 International License (CC BY 4.0).
© 2026 The Authors. Published by American Chemical Society. New and efficient chemical reactions with broad substrate applicability are needed to expand the diversity of DNA-encoded libraries (DELs), which are becoming established as a powerful technology for hit finding in medicinal chemistry. For reactions to be useful, they must be compatible with the DNA-tags and with the aqueous conditions used in DEL synthesis. One potential approach to address this requirement is the application of surfactant-mediated chemistry, which can lead to improved reaction efficiency. Our recent application of this technology to Buchwald–Hartwig aminations is very effective at coupling (hetero)aryl amines but performed less well for aliphatic substrates. This paper describes the development of an efficient, surfactant-promoted method of effecting on-DNA Buchwald–Hartwig aminations on DNA with aliphatic amines. This was developed through sequential optimization of the base, palladium ligand and the surfactant, for which Span 60 proved optimal. The applicability of the method is demonstrated across a broad substrate scope and its use in the synthesis of DELs is demonstrated by the synthesis of a prototype library.
Author(s): Carton TP, Graham JS, Waring MJ
Publication type: Article
Publication status: Published
Journal: Bioconjugate Chemistry
Year: 2026
Volume: 37
Issue: 7
Pages: 1443-1451
Print publication date: 15/07/2026
Online publication date: 02/07/2026
Acceptance date: 15/06/2026
Date deposited: 03/08/2026
ISSN (print): 1043-1802
ISSN (electronic): 1520-4812
Publisher: American Chemical Society
URL: https://doi.org/10.1021/acs.bioconjchem.6c00213
DOI: 10.1021/acs.bioconjchem.6c00213
Data Access Statement: The Supporting Information is available free of charge at https://pubs.acs.org/doi/10.1021/acs.bioconjchem.6c00213. Additional data, experimental details and supporting analytical data are available as electronic Supporting Information
PubMed id: 42390757
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