Direct heteroarylation of tautomerizable heterocycles into unsymmetrical and symmetrical biheterocycles via Pd/Cu-catalyzed phosphonium coupling |
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Authors: | Sharma Abhishek Vachhani Dipak Van der Eycken Erik |
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Institution: | Laboratory for Organic & Microwave-Assisted Chemistry, Department of Chemistry, University of Leuven, Celestijnenlaan 200F, B-3001, Leuven, Belgium. |
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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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