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Issue 20, 2019
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One-pot, modular approach to functionalized ketones via nucleophilic addition/Buchwald–Hartwig amination strategy

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Abstract

A general one-pot procedure for the 1,2-addition of organolithium reagents to amides followed by the Buchwald–Hartwig amination with in situ released lithium amides is presented. In this work amides are used as masked ketones, revealed by the addition of organolithium reagents which generates a lithium amide, suitable for subsequent Buchwald–Hartwig coupling in the presence of a palladium catalyst. This methodology allows for rapid, efficient and atom economic synthesis of aminoarylketones in good yields.

Graphical abstract: One-pot, modular approach to functionalized ketones via nucleophilic addition/Buchwald–Hartwig amination strategy

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Publication details

The article was received on 22 Oct 2018, accepted on 13 Feb 2019 and first published on 18 Feb 2019


Article type: Communication
DOI: 10.1039/C8CC08444K
Citation: Chem. Commun., 2019,55, 2908-2911

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    One-pot, modular approach to functionalized ketones via nucleophilic addition/Buchwald–Hartwig amination strategy

    J. de Jong, D. Heijnen, H. Helbert and B. L. Feringa, Chem. Commun., 2019, 55, 2908
    DOI: 10.1039/C8CC08444K

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