Evaluating N-difluoromethyltriazolium triflate as a precursor for the synthesis of high molar activity [ 18 F]fluoroform.

Autor: Pees A; Amsterdam UMC, Radiology and Nuclear Medicine, Radionuclide Center, VU University, Amsterdam, The Netherlands., Vosjan MJWD; BV Cyclotron VU, Amsterdam, The Netherlands., Chai JY; Department of Chemistry, Sogang University, Seoul, South Korea., Cha H; Department of Chemistry, Sogang University, Seoul, South Korea., Chi DY; Department of Chemistry, Sogang University, Seoul, South Korea., Windhorst AD; Amsterdam UMC, Radiology and Nuclear Medicine, Radionuclide Center, VU University, Amsterdam, The Netherlands., Vugts DJ; Amsterdam UMC, Radiology and Nuclear Medicine, Radionuclide Center, VU University, Amsterdam, The Netherlands.
Jazyk: angličtina
Zdroj: Journal of labelled compounds & radiopharmaceuticals [J Labelled Comp Radiopharm] 2021 Oct; Vol. 64 (12), pp. 466-476. Date of Electronic Publication: 2021 Sep 20.
DOI: 10.1002/jlcr.3939
Abstrakt: The trifluoromethyl group is a prominent motif in biologically active compounds and therefore of great interest for the labeling with the positron emitter fluorine-18 for positron emission tomography (PET) imaging. Multiple labeling strategies have been explored in the past; however, most of them suffer from low molar activity due to precursor degradation. In this study, the potential of 1-(difluoromethyl)-3-methyl-4-phenyl-1H-1,2,3-triazol-3-ium triflate as precursor for the synthesis of the [ 18 F]trifluoromethylation building block [ 18 F]fluoroform with high molar activity was investigated. The triazolium precursor was reacted under various conditions with [ 18 F]fluoride, providing [ 18 F]fluoroform with radiochemical yields (RCY) and molar activities (A m ) comparable and even superior with already existing methods. Highest molar activities (A m  = 153 ± 14 GBq/μmol, dc, EOS) were observed for the automated procedure on the Neptis® perform module. Due to its easy handling and good RCY and A m in the [ 18 F]fluoroform synthesis, the triazolium precursor is a valuable alternative to already known precursors.
(© 2021 The Authors. Journal of Labelled Compounds and Radiopharmaceuticals published by John Wiley & Sons Ltd.)
Databáze: MEDLINE
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