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Updated: Mar 6, 2026

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
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PPh3-Catalyzed Remote Aminofluorination Reactions: Regioselective Access to γ- and ε-Fluoroamines Containing Oxindole

Xing-Xing Dai1, Wen-Hui Zhang1, Xi-Ying Yang1

  • 1School of Pharmacy, Guizhou University of Traditional Chinese Medicine, Guiyang 550025, China.

Organic Letters
|March 4, 2026
PubMed

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Direct alkylation of ammonia produces polyalkylated amines, along with a quaternary ammonium salt. To exclusively prepare primary amines, the azide synthesis method can be used.
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Direct alkylation is not a suitable method for synthesizing amines because it produces polyalkylated products. Gabriel synthesis is the most preferred method to exclusively make primary amines. The method uses phthalimide, which contains a protected form of nitrogen that participates in alkylation only once to predominantly give primary amines.
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