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DNA-Compatible Nitro Reduction and Synthesis of Benzimidazoles
journal contribution
posted on 2017-08-25, 00:00 authored by Huang-Chi Du, Hongbing HuangDNA-encoded
chemical libraries have emerged as a cost-effective
alternative to high-throughput screening (HTS) for hit identification
in drug discovery. A key factor for productive DNA-encoded libraries
is the chemical diversity of the small molecule moiety attached to
an encoding DNA oligomer. The library structure diversity is often
limited to DNA-compatible chemical reactions in aqueous media. Herein,
we describe a facile process for reducing aryl nitro groups to aryl
amines. The new protocol offers simple operation and circumvents the
pyrophoric potential of the conventional method (Raney nickel). The
reaction is performed in aqueous solution and does not compromise
DNA structural integrity. The utility of this method is demonstrated
by the versatile synthesis of benzimidazoles on DNA.
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Benzimidazoles DNA-encoded chemical librariesDNA-Compatible Nitro Reductionaryl nitro groupslibrary structure diversityhigh-throughput screeningHTSdrug discoverymethodDNA-encoded librariescompromise DNAmolecule moietyRaney nickelDNA-compatible chemical reactionschemical diversityencoding DNA oligomeraryl amines
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