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Synthesis of [ 76 Br]4‐bromodexetimide and [ 76 Br]4‐bromolevetimide: Radiotracers for studying muscarinic cholinergic receptors using PET
Author(s) -
Kassiou Michael,
Loc'h Christian,
Strijckmans Veronique,
Katsifis Andrew,
Lambrecht Richard M.,
Maziere Mariannick,
Maziere Bernard
Publication year - 1995
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.2580360308
Subject(s) - chemistry , chloramine t , high performance liquid chromatography , radiochemistry , radiosynthesis , trimethylsilyl , bromine , biodistribution , nuclear chemistry , chromatography , medicinal chemistry , organic chemistry , positron emission tomography , in vitro , nuclear medicine , biochemistry , medicine
The muscarinic cholinergic receptor antagonist dexetimide and its pharmacologically inactive enantiomer levetimide were labelled with the positron emitter bromine‐76. [ 76 Br]4‐Bromodexetide, [ 76 Br]BrDEX, and [ 76 Br]4‐bromolevetimide, [ 76 ]BrLEV, were prepared via electrophilic bromodesilylation of 4‐(trimethylsilyl)dexetimide and 4‐(trimethyylsilyl)levetimide with [ 76 Br]NH 4 . The use of chloramine‐T in acid media resulted in radiochemical yields of 80%. The radiotracers were purified by semi‐preparative reverse‐phase HPLC. Radiochemical and chemical purities were assessed by radio‐TLC and HPLC and found to be 98%. The average time of synthesis including formulation was 60 minutes resulting in average specific activities of 300 mCi/μmol.