Randomized trial shows N-alkylation of anilines using alcohols, indicating broad applicability and functional group tolerance.
A Brønsted acid‐catalyzed methodology for the direct N ‐alkylation of anilines with alcohols has been developed. The desired products were obtained in good to excellent yields using 20 mol% of aqueous tetrafluoroboric acid as a catalyst. A broad scope of anilines and benzhydrols reacted under the developed conditions, including sterically hindered, electron‐rich, and electron‐deficient systems. Moreover, the protocol exhibits excellent functional group tolerance, such as carboxylic acid, ester, and phenol functionalities.
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Gantous et al. (2026) studied this question.
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