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Production of 18F-fluorocholine with a commercial module: First experience

¹ Operative Unit of Nuclear Medicine, La Maddalena Hospital, Palerm, Italy; ² Nuclear Medicine, IRMET S.p.A. PET Center, Torino, Italy

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Objectives: The marking of choline with 11C presents the inconvenience linked to the short half-life of 11C. Our goals are to demonstrate the feasibility, with acceptable marking yields, of the synthesis of 18Fluorometilcholine, [18F]-FCH, on a commercial synthesis module, the TracerlabFXFDG (GE), and the subsequent optimization of the synthesis process.

Methods: The synthesis of the [18F]-FCH experienced, consists of two steps: first one provides training alkylating agent, fluoromethyl bromide (18F-FCH2Br), according to the alkylation of the tertiary amine, such as N,N-dimethylaminoethanol The most difficult step is the formation of 18FCH2Br, taking place by nucleophilic substitution of CH2Br2 with 18F-previously anidrificated by two evaporation steps in presence of K2.2.2.in anhydrous acetonitrile. This intermediate is, under normal conditions, a gas, with a boiling point of 19°C, which makes it difficult to isolate for the next step. Purification is made through four silica gel Sep-Pak cartridges placed in series. 18F-FCH2Br bubbling is obtained in a solution of N,N-dimethylaminoethanol in acetonitrile at low temperatures. After this stage, we proceed to remove the solvents in excess, then the purification of [18F]-FCH.

Results: The production yield of 18F-FCH2Br starting with 18F was 25%, while the yield for [18F]-FCH was 12%. The radiochemical purity determined by HPLC was 96%. Low yields are probably due to the difficulty to trap the 18F-FCH2Br.

Conclusions: This first experience on the synthesis of [18F]-FCH has produced not optimal results(in terms of yields) but are currently going further studies to improve the methodology. Also there are going studies on the possibility to find an alternative synthesis which provides the best yields.

This Article Services Email this article to a friend Similar articles in this journal Alert me to new issues of the journal Download to citation manager Google Scholar Articles by Sperandeo, A. Articles by Ficola, U. PubMed Articles by Sperandeo, A. Articles by Ficola, U.