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Current Radiopharmaceuticals


ISSN (Print): 1874-4710
ISSN (Online): 1874-4729

Synthesis of [18F]Fallypride in a Micro-Reactor: Rapid Optimization and Multiple-Production in Small Doses for Micro-PET Studies

Author(s): Shuiyu Lu, Anthony M. Giamis and Victor W. Pike

Volume 2, Issue 1, 2009

Page: [49 - 55] Pages: 7

DOI: 10.2174/1874471010902010049

Price: $65


A commercial coiled-tube micro-reactor (NanoTek; Advion) was used as a convenient platform for the synthesis of [18F]fallypride in small doses (0.5-1.5 mCi) for micro-PET studies of brain dopamine subtype-2 receptors in rodents. Each radiosynthesis used low amounts (20-40 μg; 39-77 nmol) of tosylate precursor and [18F]fluoride ion (0.5-2.5 mCi). Optimization of the labeling reaction in the apparatus, with respect to the effects of precursor amount, reaction temperature, flow rate and [18F]fluoride ion to precursor ratio, was achieved rapidly and the decay-corrected radiochemical yield of [18F]fallypride (up to 88%) was reproducible. The low amounts of material used in each radiosynthesis allowed crude [18F]fallypride to be purified rapidly on an analytical-size reverse phase HPLC column, preceding formulation for intravenous injection. Scale-up of the reaction was easily achieved by continuously infusing reagent precursor solutions to obtain [18F]fallypride in much greater quantity.

Keywords: Micro-reactor, fluorine-18, radiofluorination, [18F]fallypride, synthesis

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