Journal
CHEMICAL COMMUNICATIONS
Volume 55, Issue 20, Pages 2908-2911Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c8cc08444k
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Funding
- European Research Council [227897]
- Netherlands Organization for Scientific Research (NOW-CW)
- Ministry of Education, Culture, and Science [024.001.035]
- Royal Netherlands Academy of Arts and Sciences (KNAW)
- NRSC-Catalysis
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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.
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