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Updated: Sep 25, 2025

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
HFIP-Promoted Selective Hydroxyalkylation of Aniline Derivatives with Arylglyoxal Hydrates
Jianguo Yang1,2, Saimei Liu1, Jing Gui2
1Collaborative Innovation Center for Advanced Organic Chemical Materials Co-Constructed by the Province and Ministry, Hubei University, Wuhan 430062, PR China.
Abstract:
A HFIP-promoted highly selective hydroxyalkylation of aniline derivatives with arylglyoxal hydrates has been realized. The reaction produces various N,N-dialkylanilines and their derivatives with α-hydroxy carbonyl units in good to excellent yields under mild conditions. Furthermore, the synthetic potential of this method has been demonstrated by the facile synthesis of several structurally interesting molecules such as benzil, 1,2,4-triazine, quinoxaline, hydantoin, and 2-thiohydantoin with aromatic amine units.
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