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Updated: Sep 13, 2025

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Additive-Free EDA Photochemical Arylative Trifluoromethylation of Enamides with Trifluoromethyl Benzothiazole
Rui Lv1, Lujun Lou1, Tianshuai Zhu1
1National Key Laboratory for the Development and Utilization of Forest Food Resources, Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, Nanjing Forestry University, Nanjing, Jiangsu 210037, China.
Abstract:
An additive-free trifluoromethylation-heteroarylation of enamides with trifluoromethyl heteroaryl sulfones via EDA photochemistry is reported. Under visible-light irradiation, diverse enamides and sulfones undergo efficient difunctionalization to afford CF3-heteroaryl amides in moderate to excellent yields, without the need for photocatalysts or additives. Mechanistic studies support the formation of a photoexcited EDA complex that triggers C-S bond cleavage, generating CF3 and heteroaryl anions. This work provides a sustainable approach to alkene arylative difunctionalization and expands the utility of aryl sulfones in constructing CF3-containing scaffolds.
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