Metal-free N-formylation of 2-aminophenols using dimethylformamide and CSA

Abstract

DMF has been proved to be an efficient formylation reagent for 2-aminophenols in the presence of (±) camphorsulfonic acid (CSA) in this work. CSA works as an acid catalyst and a neutralizer of dimethyl amine which is kicked off from DMF. Both electron-withdrawing and electron-donating groups are tolerated. More importantly, the product could be achieved in gram scale with the possibility of further diversifying into biologically interesting structures.

GRAPHICAL ABSTRACT

Keywords:

• 2-aminophenols
• camphorsulfonic acid
• formylation
• N,N-dimethylformamide

Acknowledgment

We thank BGI-Shenzhen for the support in publishing this work.

Additional information

Funding

The work was financially supported by the National Natural Science Foundation of China [21807120, 81660348, 21502030], Office of Science and Technology of Guiyang ([20151001]06).