One-pot, modular approach to functionalized ketones via nucleophilic addition/Buchwald-Hartwig amination strategyElectronic supplementary information (ESI) available: General, experimental procedures and characterisation of compounds. See DOI: 10.1039/c8cc08444k

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 lith...

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Main Authors de Jong, Jorn, Heijnen, Dorus, Helbert, Hugo, Feringa, Ben L
Format Journal Article
Published 05.03.2019
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Summary: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. A one-pot procedure for 1,2-addition of organolithium reagents to amides followed by Buchwald-Hartwig amination with in situ released lithium amides is presented.
Bibliography:Electronic supplementary information (ESI) available: General, experimental procedures and characterisation of compounds. See DOI
10.1039/c8cc08444k
ISSN:1359-7345
1364-548X
DOI:10.1039/c8cc08444k