Direct Amination of Aromatic Boronic Acids with Aqueous Ammonia

Significance

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.