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Synthesis of Unsymmetrical 2,6-Diarylanilines by Palladium-Catalyzed C–H Bond Functionalization Methodology

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journal contribution
posted on 07.05.2018, 11:48 authored by Se Hun Kwak, Nurbey Gulia, Olafs Daugulis
3,5-Dimethylpyrazole was employed as a monodentate directing group for palladium-catalyzed ortho-sp2 C–H arylation with aryl iodides. The reaction shows good functional group tolerance and outstanding selectivity for mono-ortho-arylation. Ozonolysis of ortho-arylated arylpyrazoles gave acylated biphenylamines that were further arylated to afford unsymmetrically substituted 2,6-diarylacetanilides.