We herein describe
a practical direct amination of phenols through
a palladium-catalyzed hydrogen-transfer-mediated activation method
to synthesize the secondary and tertiary amines. In this conversion,
environmentally friendly water and inexpensive ammonium formate were
used as solvent and reductant, respectively. A range of amines, including
aliphatic amines, aniline, secondary amines, and diamines, could be
coupled effectively by this method to achieve mono/dual amination
and cyclization of phenols. This study not only provides a green and
mild strategy for the synthesis of secondary and tertiary naphthylamines
but also expands the synthesis of chloroquine in organic chemistry.