18F fluoroethylations: different strategies for the rapid translation of 11C-methylated radiotracers

Author(s)
Wolfgang Wadsak, Leonhard-Key Mien, Dagmar E. Ettlinger, Harald Eidherr, Daniela Haeusler, Karoline Maria Sindelar, Bernhard Keppler, Robert Dudczak, Kurt Kletter, Markus Mitterhauser
Abstract

Introduction: The translation of 11C-labeled compounds into their respective 18F-labeled derivatives is an important tool in the rapid development of positron emission tomography (PET) tracers. Thus, our aim was the development of a general method for the preparation of 18F-fluoroethylated compounds that (a) is applicable to a variety of precursors, (b) can be performed in a fully automated commercially available synthesizer and (c) enables this rapid translation of 11C-methylated tracers into their 18F-fluoroethylated analogs sharing the same precursor molecules. Methods: Ten methods for the preparation and purification of different 18F-fluoroethylating agents were compared. Subsequently, five 18F-labeled PET tracers were synthesized under fully automated conditions. Results: Radiochemical yields ranged from 34.4% to 60.8%, and time consumption ranged from 20 to 55 min for all methods. Use of 1-bromo-2-[18F]fluoroethane and distillation evinced as the method of choice. Conclusions: We were able to develop a general method for the preparation of a variety of 18F-fluoroethylated molecules. The provided tool is solely based on commercially available resources and has the potential to simplify and accelerate innovative PET tracer development in the future. © 2007 Elsevier Inc. All rights reserved.

Organisation(s)
Department of Inorganic Chemistry
External organisation(s)
Medizinische Universität Wien
Journal
Nuclear Medicine and Biology
Volume
34
Pages
1019-1028
No. of pages
10
ISSN
0969-8051
DOI
https://doi.org/10.1016/j.nucmedbio.2007.06.012
Publication date
2007
Peer reviewed
Yes
Austrian Fields of Science 2012
104003 Inorganic chemistry
Portal url
https://ucrisportal.univie.ac.at/en/publications/7776875b-5aaf-4d93-b114-0b75f06312d9