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Radiosynthesis of [11C]SL25.1188 via [11C]CO2 fixation for imaging monoamine oxidase B

✍ Scribed by Neil Vasdev; Oleg Sadovski; Armando Garcia; Frédéric Dollé; Jeffrey H. Meyer; Sylvain Houle; Alan A. Wilson

Publisher
John Wiley and Sons
Year
2011
Tongue
French
Weight
153 KB
Volume
54
Category
Article
ISSN
0022-2135

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✦ Synopsis

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.

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