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Issue 10, 2019
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Innate pharmacophore assisted selective C–H functionalization to therapeutically important nicotinamides

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Abstract

The application of the pre-validated pharmacophore 2-(2-oxazolinyl)aniline as an innate directing group in the C–H etherification and amination of nicotinamides for the efficient synthesis of drug- and agrochemical-like molecules was determined. An operationally simple, and regioselective C–H functionalization of nicotinamides was first accomplished using a complicated variation of copper salts. All the specific procedures used were easy to utilize, without external oxidants or ligands. The feasibility is highlighted using an alternative synthesis of diflufenican with a rapid synthesis of niacin related pharmaceuticals or analogues.

Graphical abstract: Innate pharmacophore assisted selective C–H functionalization to therapeutically important nicotinamides

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Publication details

The article was received on 16 Feb 2019, accepted on 23 Mar 2019 and first published on 25 Mar 2019


Article type: Research Article
DOI: 10.1039/C9QO00170K
Org. Chem. Front., 2019,6, 1613-1618

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    Innate pharmacophore assisted selective C–H functionalization to therapeutically important nicotinamides

    Z. Song, G. Wang, W. Li and S. Li, Org. Chem. Front., 2019, 6, 1613
    DOI: 10.1039/C9QO00170K

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