Radiosynthesis of [11C]SL25.1188 via [11C]CO2 fixation for imaging monoamine oxidase B
作者： Neil Vasdev , Oleg Sadovski , Armando Garcia , Frédéric Dollé , Jeffrey H. Meyer
DOI: 10.1002/JLCR.1908
关键词:
摘要: Carbon-11-labelled (S)-5-methoxymethyl-3-[6-(4,4,4-trifluorobutoxy)benzo[d]isoxazol-3-yl]oxazolidin-2-[11C]-one ([11C]SL25.1188), a promising reversibly binding radiotracer for imaging central monoamine oxidase B, was rapidly prepared via an intramolecular cyclization reaction in automated one-pot procedure directly from [11C]CO2, thereby precluding the use of [11C]COCl2. Formulated [11C]SL25.1188 isolated 12 ± 1% uncorrected radiochemical yield, based on starting with specific activity 37 ± 2 GBq/µmol at end synthesis (30 min; n = 3). Radiochemical and enantiomeric purities were both >99%. The methodology described herein offers efficient production ambient temperature is suitable human studies.
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