Radiosynthesis of [5-[11C]methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-[5-(tetrahydro-pyran-4-yl)-1,3-dihydro-isoindol-2-yl]-methanone ([11C]RO5013853), a novel PET tracer for the glycine transporter type I (GlyT1)
✍ Scribed by Emmanuel Pinard; Serge Burner; Philipp Cueni; Thomas Hartung; Roger D. Norcross; Philipp Schmid; Pius Waldmeier; Guy Zielinski; Hayden T. Ravert; Daniel P. Holt; Robert F. Dannals
- Publisher
- John Wiley and Sons
- Year
- 2011
- Tongue
- French
- Weight
- 300 KB
- Volume
- 54
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
The glycine transporter type 1 (GlyT1) has emerged as a key novel target for the treatment of schizophrenia. We have recently discovered and developed [^11^C]RO5013853 as a novel positron emission tomography tracer for GlyT1 for which a reliable five‐step synthetic route was established. The incorporation of the radioisotope was achieved in the final step through methylation of a sodium sulfinate precursor, itself easily accessible upon reduction of the corresponding sulfonyl‐chloride analog. [^11^C]RO5013853 was prepared with high specific activity (>49 GBq/µmol) and high radiochemical purity (100%). A validation study of [^11^C]RO5013853 in animal imaging studies is in progress. Copyright © 2011 John Wiley & Sons, Ltd.