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Updated: Jan 14, 2026

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Controllable Phosphorothiotrifluoromethylation and Hydrotrifluoromethylation of Unactivated Alkenes in Water
Chi Gao1, Hongye Zhu1, Cong Xu1
1Jilin Province Key Laboratory of Organic Functional Molecular Design & Synthesis, College of Chemistry, Northeast Normal University, Changchun 130024, China.
Abstract:
Metal-free redox strategy provides an efficient and simple mode for the difunctionalization of olefins, but is not well used for trifluoromethyl-sufuration mainly because such a process is accompanied by many competitive reactions. Here, we report two selective alkene difunctionalizations, phosphorothiotrifluoromethylation and hydrotrifluoromethylation, by taming a three-component redox reaction under metal-free conditions. The method features greenness, operational simplicity, high efficiency, gram-scale synthesis, and late-stage functionalization, and is also applicable to corresponding perfluoroalkylation-based reactions.
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