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Updated: Aug 9, 2025

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
N-Trifluoromethyl Succinimide as a New Reagent for Direct C-H Trifluoromethylation of Free Anilines
Hao Liu1, Xin He1, Zhicheng Chen1
1School of Chemistry and Materials Science, Heilongjiang University, Harbin, Heilongjiang, 150080, P. R. China.
Abstract:
N-trifluoromethylsuccinimide (NTFS) as a new trifluoromethylation reagent was designed and prepared via Ag-CF3 , and applied to the direct trifluoromethylation of free aniline, and a series of trifluoromethyl products were obtained with good yields. The practicability of the protocol was verified by a gram-level experiment and the synthesis of the antiasthmatic drug Mabuterol. In addition, a possible radical mechanism was proposed and verified by related experiments. The protocol provided a new solution for C-H trifluoromethylation of free anilines.
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