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Updated: May 27, 2025

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Photocatalytic C-H Trifluoroethoxylation of (Hetero)arenes
Mingxi Chen1, Jingjing Ling1, Keguang Cheng1,2
1State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China), Collaborative Innovation Center for Guangxi Ethnic Medicine, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin, Guangxi 541004, P. R. China.
Abstract:
The trifluoroethoxy group (OCH2CF3) is a valuable motif prevalent in pharmaceuticals and agrichemicals. Herein, we present a simple radical trifluoroethoxylation method that enables nondirected functionalization of C-H bonds of a broad array of substrates, providing access to (hetero)aryl trifluoroethyl ethers. The current protocol tolerates a variety of synthetically and pharmacologically relevant functional groups. Applicability is also demonstrated through the late-stage functionalization of biorelevant molecules and marketing drugs.
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