TY - JOUR
T1 - Evaluating N-difluoromethyltriazolium triflate as a precursor for the synthesis of high molar activity [18F]fluoroform
AU - Pees, Anna
AU - Vosjan, Maria J. W. D.
AU - Chai, Jin Young
AU - Cha, Hyojin
AU - Chi, Dae Yoon
AU - Windhorst, Albert D.
AU - Vugts, Danielle J.
N1 - Funding Information: The project is financially supported by the Dutch Research Council (NWO) Grant 731.015.413 and BV Cyclotron VU (beneficiary: D. Vugts) and by The Radiation Technology R&D program through the National Research Foundation of Korea funded by the Ministry of Science, ICT & Future Planning (2016M2A2A7A03913537) (beneficiary: D. Y. Chi). Publisher Copyright: © 2021 The Authors. Journal of Labelled Compounds and Radiopharmaceuticals published by John Wiley & Sons Ltd. Copyright: Copyright 2021 Elsevier B.V., All rights reserved.
PY - 2021/10
Y1 - 2021/10
N2 - 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 [18F]trifluoromethylation building block [18F]fluoroform with high molar activity was investigated. The triazolium precursor was reacted under various conditions with [18F]fluoride, providing [18F]fluoroform with radiochemical yields (RCY) and molar activities (Am) comparable and even superior with already existing methods. Highest molar activities (Am = 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 Am in the [18F]fluoroform synthesis, the triazolium precursor is a valuable alternative to already known precursors.
AB - 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 [18F]trifluoromethylation building block [18F]fluoroform with high molar activity was investigated. The triazolium precursor was reacted under various conditions with [18F]fluoride, providing [18F]fluoroform with radiochemical yields (RCY) and molar activities (Am) comparable and even superior with already existing methods. Highest molar activities (Am = 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 Am in the [18F]fluoroform synthesis, the triazolium precursor is a valuable alternative to already known precursors.
KW - [ F]fluoroform
KW - [ F]trifluoromethylation
KW - fluorine-18
KW - high molar activity
KW - triazolium precursor
UR - http://www.scopus.com/inward/record.url?scp=85115153642&partnerID=8YFLogxK
U2 - https://doi.org/10.1002/jlcr.3939
DO - https://doi.org/10.1002/jlcr.3939
M3 - Article
C2 - 34382259
SN - 0362-4803
VL - 64
SP - 466
EP - 476
JO - Journal of Labelled Compounds and Radiopharmaceuticals
JF - Journal of Labelled Compounds and Radiopharmaceuticals
IS - 12
ER -