Efficient copper-catalyzed amination of DNA-conjugated aryl iodides under mild aqueous conditions

Yves Ruff; Frédéric Berst
Med. Chem. Commun., 2018, 9, 1188-1193
https://doi.org/10.1039/C8MD00185E

Abstract

Herein, we describe the development of a copper-catalyzed amination of DNA-conjugated aryl iodides with aliphatic amines. This protocol leverages a novel ligand, 2-((2,6-dimethoxyphenyl)amino)-2-oxoacetic acid, to effect the transformation in aqueous DMSO, under mild conditions, in air, making it an ideal candidate for the synthesis of DNA-encoded libraries.

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