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Two‐step radiosynthesis of [ 18 F]FE‐ β ‐CIT and [ 18 F]PR04.MZ
Author(s) -
Riss Patrick J.,
Hoehnemann Sabine,
Piel Markus,
Roesch Frank
Publication year - 2013
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3032
Subject(s) - chemistry , radiosynthesis , yield (engineering) , octane , reagent , medicinal chemistry , radiochemistry , nuclear chemistry , carboxylic acid , organic chemistry , in vivo , materials science , microbiology and biotechnology , metallurgy , biology
The cocaine‐derived dopamine reuptake inhibitors FE‐ β ‐CIT (8‐(2‐fluoroethyl)‐3‐(4‐iodophenyl)‐8‐azabicyclo[3.2.1]octane‐2‐carboxylic acid methyl ester) (1) and PR04.MZ(8‐(4‐fluorobut‐2‐ynyl)‐3‐p‐tolyl‐8‐azabicyclo[3.2.1]octane‐2‐carboxylic acid methyl ester) (2) were labelled with 18 F‐fluorine using a two‐step route. 2‐[ 18 F]Fluoroethyltosylate and 4‐[ 18 F]fluorobut‐2‐yne‐1‐yl tosylate were used as labelling reagents, respectively. Radiochemically pure (>98%) [ 18 F]FE‐ β ‐CIT and [ 18 F]PRD04.MZ (32–86 GBq/µmol) were obtained after a synthesis time of 100 min in about 25% non‐decay‐corrected overall yield.