Synfacts 2006(10): 1055-1055  
DOI: 10.1055/s-2006-949307
Metal-Mediated Synthesis
© Georg Thieme Verlag Stuttgart · New York

A Mild Copper-Catalyzed Amination of Haloarenes

Contributor(s): Paul Knochel, Andrei Gavryushin
A. Shafir, S. L. Buchwald*
Massachusetts Institute of Technology, Cambridge, USA
Further Information

Publication History

Publication Date:
21 September 2006 (online)

Significance

The direct amination of aryl halides is the most straightforward method for the preparation of polysubstituted anilines. While a number of highly efficient catalytic procedures has already been described, the development of new mild and versatile protocols for this transformation is a challenging task. Herein, the authors describe a new version of Cu-catalyzed amination of aryl bromides and iodides, which uses diketones, a rather unusual class of ligands for metal catalysis. The procedure is very simple, does not require harsh conditions or expensive catalysts and offers uniformly high yields of products.