Synthesis of [18F]Fluoroform with High Molar Activity

Anna Pees*, Albert D. Windhorst, Maria J.W.D. Vosjan, Vincent Tadino, Danielle J. Vugts

*Corresponding author for this work

Research output: Contribution to journalArticleAcademicpeer-review

Abstract

Fluoroform is an interesting motif for the isotopologue labelling of biologically active compounds with fluorine-18 for PET imaging. However, so far the building block [18F]fluoroform and consequently the [18F]trifluoromethylated products suffered from low molar activities ranging from 0.1 to 30 GBq/µmol due to isotopic dilution under the strongly basic standard radiofluorination conditions. In this article the synthesis of high molar activity [18F]fluoroform is described. By implementing a recently reported novel radiofluorination reagent, [18F]triflyl fluoride, the concentration of base-cryptand complex in the reaction could be reduced 100-fold compared to standard radiofluorination conditions and molar activities close to 100 GBq/µmol (at end of [18F]fluoroform synthesis) could be obtained, enabling the imaging of low density receptors. Furthermore, an automated procedure was developed on the commercially available NEPTIS® perform synthesizer to provide access of high molar activity [18F]fluoroform to other PET centres.

Original languageEnglish
Pages (from-to)1177-1185
Number of pages9
JournalEuropean Journal of Organic Chemistry
Volume2020
Issue number9
DOIs
Publication statusPublished - 8 Mar 2020

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