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Ligand-Free Copper-Catalyzed Arylation of Amidines

Michelle Cortes-Salva, Corey Garvin and Jon C. Antilla*

*Department of Chemistry, University of South Florida, 4202 East Fowler Avenue CHE 205A, Tampa, Florida 33620, United States, Email:

M. Cortes-Salva, C. Garvin, J. C. Antilla, J. Org. Chem., 2011, 76, 1456-1459.

DOI: 10.1021/jo102235u


Copper-catalyzed cross-coupling reactions of amidine salts with aryl iodides give monoarylated amidines in good yields under ligand-free conditions. DMF was the superior solvent for the N-arylation of benzamidines, while MeCN was used in the formation of N-aryl amidines in good yield.

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Key Words

Ullmann Coupling, Amidines

ID: J42-Y2011-0480