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Copper-Catalyzed Oxidative Three-Component Synthesis of N,N′,N″-Trisubstituted Guanidines

Jihui Li and Luc Neuville *

*Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, Laboratoire International Associť, CNRS, 91198 Gif-sur-Yvette Cedex, France, Email:

J. Li, L. Neuville, Org. Lett., 2013, 15, 6124-6127.

DOI: 10.1021/ol4029622

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An operationally simple and rapid copper-catalyzed three-component synthesis of trisubstituted N-aryl guanidines involving cyanamides, arylboronic acids, and amines is performed in the presence of K2CO3, a catalytic amount of CuCl2∑2H2O, bipyridine, and oxygen (1 atm).

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Key Words

Condensation, N-Functionalization, Oxygen, Multicomponent Reactions

ID: J54-Y2013