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Heavy metal orchestration

Many current methods to prepare 2-hydroxybiaryls require the prefunctionalization of phenol groups or show limited substrate scope. Now, use of a pentavalent sulfone-bridged bismacycle, formed in situ by telescoped boron-to-bismuth transmetallation and oxidation, allows the direct and regioselective ortho-arylation of unprotected phenols.

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Fig. 1: Development of a general method for the direct and regioselective ortho-arylation of unprotected phenols via a telescoped one-pot boron-to-bismuth transmetallation and oxidation sequence.


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Correspondence to Alexandre Gagnon.

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Le Roch, A., Gagnon, A. Heavy metal orchestration. Nat. Chem. 12, 223–224 (2020).

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