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

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Novartis Institutes for BioMedical Research, Novartis Pharma AG , Novartis Campus , 4002 Basel , Switzerland . Email:

Published: July 2018

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.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6072498PMC
http://dx.doi.org/10.1039/c8md00185eDOI Listing

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