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

Identifieur interne : 000302 ( Istex/Corpus ); précédent : 000301; suivant : 000303

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

Auteurs : Neil Vasdev ; Oleg Sadovski ; Armando Garcia ; Frédéric Dollé ; Jeffrey H. Meyer ; Sylvain Houle ; Alan A. Wilson

Source :

RBID : ISTEX:72E33E45E4BB7A9B3D56F08E0CEE2BEF984EC951

Abstract

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 an automated one‐pot procedure directly from [11C]CO2, thereby precluding the use of [11C]COCl2. Formulated [11C]SL25.1188 was isolated in 12 ± 1% uncorrected radiochemical yield, based on starting [11C]CO2, 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 [11C]SL25.1188 at ambient temperature and is suitable for human imaging studies.

Url:
DOI: 10.1002/jlcr.1908

Links to Exploration step

ISTEX:72E33E45E4BB7A9B3D56F08E0CEE2BEF984EC951

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