[(18)F]fluoride Activation and (18)F-Labelling in Hydrous Conditions-Towards a Microfluidic Synthesis of PET Radiopharmaceuticals

在水合条件下对氟化物进行活化和标记——迈向PET放射性药物的微流控合成

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Abstract

(18)F-labelled radiopharmaceuticals are indispensable in positron emission tomography. The critical step in the preparation of (18)F-labelled tracers is the anhydrous F-18 nucleophilic substitution reaction, which involves [(18)F]F(-) anions generated in aqueous media by the cyclotron. For this, azeotropic drying by distillation is widely used in standard synthesisers, but microfluidic systems are often not compatible with such a process. To avoid this step, several methods compatible with aqueous media have been developed. We summarised the existing approaches and two of them have been studied in detail. [(18)F]fluoride elution efficiencies have been investigated under different conditions showing high (18)F-recovery. Finally, a large scope of precursors has been assessed for radiochemical conversion, and these hydrous labelling techniques have shown their potential for tracer production using a microfluidic approach, more particularly compatible with iMiDEV™ cassette volumes.

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