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Issue 8, 2017
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On-DNA Pd and Cu promoted C–N cross-coupling reactions

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Abstract

Encoded library technology (ELT) is a novel hit identification platform synergistic with HTS, fragment hit ID and focused screening. It provides both an ultra high-throughput and a cost-efficient tool for the discovery of small molecules that bind to protein targets of pharmaceutical interest. The success of ELT relies heavily on the chemical diversity accessed through DNA-encoded library (DEL) synthesis. We developed unprecedented Pd and Cu(I) promoted C–N cross-coupling reactions between a DNA-conjugated aryl iodide and primary amines. These reported reactions have strong potential for application in DNA-encoded library (DEL) synthesis.

Graphical abstract: On-DNA Pd and Cu promoted C–N cross-coupling reactions

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Publication details

The article was received on 03 Jun 2017, accepted on 11 Jul 2017 and first published on 12 Jul 2017


Article type: Research Article
DOI: 10.1039/C7MD00289K
Citation: Med. Chem. Commun., 2017,8, 1614-1617
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    On-DNA Pd and Cu promoted C–N cross-coupling reactions

    X. Lu, S. E. Roberts, G. J. Franklin and C. P. Davie, Med. Chem. Commun., 2017, 8, 1614
    DOI: 10.1039/C7MD00289K

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