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Issue 7, 2018
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Efficient copper-catalyzed amination of DNA-conjugated aryl iodides under mild aqueous conditions

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Abstract

Herein, we describe the development of copper-catalyzed cross-coupling 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 and in air, making it an ideal candidate for the synthesis of DNA-encoded libraries.

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

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Publication details

The article was received on 04 Apr 2018, accepted on 17 May 2018 and first published on 17 May 2018


Article type: Research Article
DOI: 10.1039/C8MD00185E
Citation: Med. Chem. Commun., 2018,9, 1188-1193

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

    Y. Ruff and F. Berst, Med. Chem. Commun., 2018, 9, 1188
    DOI: 10.1039/C8MD00185E

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