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Updated: Jun 15, 2025

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
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Redox-Active α-Amino-CF3 Reagents: Developing and Applications in Ni-Catalyzed Reductive Cross-Coupling
Yifan Ni1, Ying Wang2, Jiyang Liu1
1State Key Laboratory of Coordination Chemistry, MOE Key Laboratory of High Performance Polymer Materials and Technology, Jiangsu Key Laboratory of Advanced Organic Materials, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing 210023, China.
Abstract:
α-Amino-CF3 compounds are widely employed in bio- and pharmaceutical chemistry for improved stability and bioactivities. Traditional methods often face challenges with functional group tolerance and lack a general approach for late-stage functionalization. Herein, we report a new type of redox-active α-amino-CF3 reagents, easily prepared from trifluoro acetaldehyde hydrates. These α-amino-CF3 reagents can serve as versatile building blocks for coupling with alkynyl bromides, aryl bromides, and enol triflates under nickel catalysis.
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