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Radiosynthesis of [ 11 C]SL25.1188 via [ 11 C]CO 2 fixation for imaging monoamine oxidase B
Author(s) -
Vasdev Neil,
Sadovski Oleg,
Garcia Armando,
Dollé Frédéric,
Meyer Jeffrey H.,
Houle Sylvain,
Wilson Alan A.
Publication year - 2011
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.1908
Subject(s) - chemistry , yield (engineering) , radiosynthesis , monoamine oxidase b , radiochemistry , specific activity , monoamine oxidase , nuclear chemistry , enantiomer , stereochemistry , medicinal chemistry , enzyme , nuclear medicine , organic chemistry , positron emission tomography , medicine , materials science , metallurgy
Carbon‐11‐labelled ( S )‐5‐methoxymethyl‐3‐[6‐(4,4,4‐trifluorobutoxy)benzo[ d ]isoxazol‐3‐yl]oxazolidin‐2‐[ 11 C]‐one ([ 11 C]SL25.1188), a promising reversibly binding radiotracer for imaging central monoamine oxidase B, was rapidly prepared via an intramolecular cyclization reaction in an automated one‐pot procedure directly from [ 11 C]CO 2 , thereby precluding the use of [ 11 C]COCl 2 . Formulated [ 11 C]SL25.1188 was isolated in 12 ± 1% uncorrected radiochemical yield, based on starting [ 11 C]CO 2 , with a specific activity of 37 ± 2 GBq/µmol at the end of synthesis (30 min; n = 3). Radiochemical and enantiomeric purities were both >99%. The methodology described herein offers an efficient production of [ 11 C]SL25.1188 at ambient temperature and is suitable for human imaging studies.