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Ruthenium-Mediated N‑Arylation for DNA-Encoded Libraries

Title Ruthenium-Mediated N‑Arylation for DNA-Encoded Libraries
Authors Suraj Kanoo, Eduardo de Pedro Beato, Tim Schulte, Lara Vogelsang, Luca Torkowski, Felix Waldbach, Philipp Hartmann, Riya Kayal, Karl-Josef Dietz, Tobias Ritter
Magazine Journal of the American Chemical Society
Date 09/11/2025
DOI https://doi.org/10.1021/jacs.5c11842
Introduction C–N cross coupling reactions are essential for forming carbon–nitrogen bonds, but achieving chemoselectivity with amino functionalities in oligonucleotides remains challenging. This study introduces a novel ruthenium reagent that facilitates selective N-arylation of amine–DNA conjugates, differing from traditional palladium-based catalysts. The reagent uses η6 π-arene coordination to activate haloarenes in situ for subsequent S NAr with the amine. It is compatible with various haloarenes and aliphatic amines, operating under mild conditions.
Quote Suraj Kanoo, Eduardo de Pedro Beato and Tim Schulte et al. Ruthenium-Mediated N‑Arylation for DNA-Encoded Libraries. J. Am. Chem. Soc. 2025. Vol. 147(38):35011-35018. DOI: 10.1021/jacs.5c11842
Element Ruthenium (Ru)
Materials Chemical Compounds
Industry Chemical & Pharmacy , Research & Laboratory
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