Synfacts 2016; 12(10): 1071
DOI: 10.1055/s-0036-1589202
Metal-Mediated Synthesis
© Georg Thieme Verlag Stuttgart · New York

Aromatic Hydroxylation and Amination through Deprotonative Cupration

Paul Knochel
Marthe Ketels
Tezuka N, Shimojo K, Hirano K, * Komagawa S, Yoshida K, Wang C, Miyamoto K, Saito T, Takita R, Uchiyama M. * The University of Tokyo and RIKEN Center for Sustainable Resource Science, Saitama, Japan
Direct Hydroxylation and Amination of Arenes via Deprotonative Cupration.

J. Am. Chem. Soc. 2016;
138: 9166-9171
Further Information

Publication History

Publication Date:
19 September 2016 (online)



The authors report an efficient aromatic hydroxylation and amination reaction through directed ortho cupration. The method is applicable to a wide range of functionalized aromatic and heteroaromatic compounds, and shows high chemo- and regioselectivity.



The reported reaction is the first example of an efficient, one-pot synthesis of functionalized phenols and anilines from the same substrates.