Abstract
Based on the direct nucleophilic aromatic substitution described previously for [ 18 F]N- methylspiperone the butyrophenone neuroleptics benperidol, droperidol, fluanisone and haloperidol were labelled with fluorine-18. The n.c.a. aromatic nucleophilic NO 2 → 18F substitution takes place in the presence of the moderately basic cryptate system consisting of Kryptofix® 2.2.2., potassium oxalate and potassium carbonate. The one step labeling reaction was performed in different solvents and is equally successful in dimethylsulfoxide, dimethylformamide or dimethylacetamide yielding 25–35% (EOS) within a reaction time of 5–30 min in the range of 140–160°C at analytical activity levels.
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