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Updated: Feb 20, 2026

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Visible-light-induced C-H trifluoromethylation of several nitrogen heterocycles with CF3Br
Yuyu Lv1, Zhijun Zhu1, Xiaopeng Hai1
1College of Chemistry and Chemical Engineering, Northwest Normal University, 967 Anning East Road, Lanzhou 730070, China. huyl@nwnu.edu.cn.
Abstract:
A visible-light-induced effective strategy for C-H trifluoromethylation of several nitrogen heterocycles with CF3Br in the presence of 3DBA2FBN and K2CO3 has been developed, which efficiently provided trifluoromethylated nitrogen heterocycles, including indoles, imidazoles, indazoles, uracils, quinazolinones, quinoxalinones, pirfenidone, pentoxifylline, caffeine and theophylline, in good yields under mild conditions. In particular, the industrially available and cheap CF3Br is used as a trifluoromethylation reagent in this process, endowing the process with the potential to be used on a large scale. The mechanism was proposed based on the control experiments. The protocol also has the advantages of good prospects for industrial applications, broad substrate scope and green energy sources.
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