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  • Title: Direct heteroarylation of tautomerizable heterocycles into unsymmetrical and symmetrical biheterocycles via Pd/Cu-catalyzed phosphonium coupling.
    Author: Sharma A, Vachhani D, Van der Eycken E.
    Journal: Org Lett; 2012 Apr 06; 14(7):1854-7. PubMed ID: 22416815.
    Abstract:
    The direct cross-coupling of tautomerizable heterocycles with various unfunctionalized heteroarenes has been achieved through PyBroP-mediated and Pd/Cu-catalyzed sequential C-OH/C-H activation. The methodology allows a facile entry into novel diazine-azole biheterocyclic frameworks. Moreover, an unprecedented Pd-catalyzed phosphonium homocoupling of tautomerizable heterocycles was also developed to afford a direct synthetic route to symmetrical 1,2-, 1,3-, and 1,4-bidiazine units.
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