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Updated: Jan 11, 2026

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
ortho-C-O arylation of aromatic amides with Grignard reagents through the Meyers reaction
Ya Wu1,2, Bohao Wang1,2, Yiran Shi1
1School of Chemistry and Chemical Engineering, Northwestern Polytechnical University, Xi'an 710072, China. liupei@nwpu.edu.cn.
Abstract:
ortho-C-O arylation of arylamides is a step-efficient and straightforward approach for the construction of biphenyl amides, yet achieving it in practice remains a great challenge. Herein, we address this challenge by developing an efficient ortho-C-O arylation of various aryl amides with Grignard reagents through a Meyers-type reaction mechanism, performed in the absence of transition-metal catalysts. This protocol enables the selective synthesis of diverse biphenyl amides, featuring high yields and broad substrate scope.
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