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Updated: Mar 27, 2026

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Nickel-Catalyzed Aminocarbonylation of Aryl Trifluoromethoxides
Zhen-Wei Liu1,2, Chang-Sheng Kuai1, Xiao-Feng Wu1,2
1Dalian National Laboratory for Clean Energy, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, China.
Abstract:
Aryl trifluoromethoxides (ArOCF3) are widely employed in pharmaceuticals and agrochemicals, which leads to their transformation also being attractive. Here we report a nickel-catalyzed aminocarbonylation of ArOCF3 with amines using inositol hexaformate (HFI) as the CO source, providing a potential approach for the chemical upcycling of these persistent compounds into value-added benzamide derivatives. The reaction exhibits broad compatibility with diverse aniline derivatives, accommodating various electronic and steric demands. This work not only expands the aryl source for amide synthesis from conventional electrophiles to the highly robust ArOCF3 motif but also offers a blueprint for phenol activation.
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