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Direct Guanidinylation of Aryl and Heteroaryl Halides via Copper-Catalyzed Cross-Coupling Reaction

Hassan Hammoud, Martine Schmitt*, Frédéric Bihel, Cyril Antheaume and Jean-Jacques Bourguignon

*Laboratoire d'Innovation Thérapeutique, UMR 7200, Faculté de pharmacie, Université de Strasbourg, 74 route du Rhin, BP 60024, 67401 Illkirch, France, Email:

H. Hammoud, M. Schmitt, F. Bihel, C. Antheaume, J.-J. Bourguignon, J. Org. Chem., 2012, 77, 417-423.

DOI: 10.1021/jo202018w


A modified Ullmann reaction allows the use of p-methoxybenzyl (PMB) guanidine as guanidinylation agent to give various aryl and heteroaryl guanidines in good yields.

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ID: J42-Y2012-0040