Issue 7, 2018

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

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

Supplementary files

Article information

Article type
Research Article
Submitted
04 Apr 2018
Accepted
17 May 2018
First published
17 May 2018

Med. Chem. Commun., 2018,9, 1188-1193

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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