Cu-mediated selective bromination of aniline derivatives and preliminary mechanism study

Abstract

A simple and efficient bromination of aniline, aniline derivatives, and analogs have been developed. Forty three examples were given and the highest yield reached was 98%. Different substrates including substituted aniline, pyridin-amine, N-substituted aniline, N,N-disubstituted aniline, N-phenyl-amide, N-phenyl-sulfonamide, and nitrogen-containing heterocycles were all reactive and selectively generated desired bromo-products. The method can be applied to synthesize drug intermediate and quinoxaline derivatives.

Graphical Abstract

KEYWORDS:

• Bromination
• copper
• aniline
• ambroxol
• quinoxaline

Additional information

Funding

Financial support from The National Natural Science Foundation of China (Grant No. 81673354) is gratefully acknowledged.