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

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• 作者：Wolfgang Wadsak ; Leonhard-Key Mien ; Dagmar E. Ettlinger ; Harald Eidherr ; Daniela Haeusler ; Karoline-Maria Sindelar ; Bernhard K. Keppler ; Robert Dudczak ; Kurt Kletter ; Markus Mitterhauser
• 关键词：PET ; Fluorine-18 ; FETO ; Fluoroethylation
• 刊名：Nuclear Medicine and Biology
• 出版年：2007
• 出版时间：November 2007
• 年：2007
• 卷：34
• 期：8
• 页码：1019-1028
• 全文大小：1016 K

文摘

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.