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Updated: Feb 18, 2026

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Organocatalyst-assisted Ar-18F bond formation: a universal procedure for direct aromatic radiofluorination
Jimmy Erik Jakobsson1, Gaute Grønnevik, Patrick Johannes Riss
1Realomics Strategic Research Initiative, Department of Chemistry, Faculty for Mathematics and Natural Sciences, University of Oslo, Norway. Patrick.Riss@kjemi.uio.no.
Abstract:
A metal free, phosphane-catalysed protocol for C-F bond formation based on ipso-elimination of iodanes is described. The reaction proceeds in significantly higher yield and with markedly reduced variability of yields (yield range) than previously described procedures. Rapid and efficient radiofluorination is achieved using unobjectionable chemical reagents with precedence in routine radiotracer production. With operational ease and mild conditions, the method promises a high potential for radiolabelling of biomolecules.
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