Synfacts 2009(4): 0433-0433  
DOI: 10.1055/s-0028-1087827
Metal-Mediated Synthesis
© Georg Thieme Verlag Stuttgart ˙ New York

Direct Amination of Aromatic Boronic Acids with Aqueous Ammonia

Contributor(s): Paul Knochel, Tobias Thaler
H. Rao, H. Fu*, Y. Jiang, Y. Zhao
Tsinghua University, Beijing, P. R. of China
Further Information

Publication History

Publication Date:
23 March 2009 (online)


The direct copper-catalyzed amination of (hetero)arylboronic acids with aqueous ammonia constitutes a new economical and highly expedient method for the introduction of an NH2 group. This reaction displays a remarkable functional group tolerance, that does not only allow the conversion of arylboronic acids bearing highly sensitive groups such as nitro and aldehyde groups, but also highly acidic functionalities. The reaction proceeds under air at room temperature which makes it an exceedingly convenient procedure for practical handling.