Organic Chemistry

Synthesis of Benzofuropyridines and Dibenzofurans by a Metalation/Negishi Cross-Coupling/SNAr Reaction Sequence



An efficient methodology for the synthesis of benzofuropyridines and dibenzofurans from fluoropyridines or fluoroarenes and 2-bromophenyl acetates is reported. This streamlined one-pot procedure consists of a four-step directed ortho-lithiation, zincation, Negishi cross-coupling, and intramolecular nucleophilic substitution, allowing for the facile assembly of a diverse set of fused benzofuro heterocycles.


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Supplementary material

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Supporting Information
The Supporting Information for this article contain experimental procedures and characterisation data for all new compounds, copies of 1H, 13C and 19F NMR spectra as well as crystallographic data.