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Optimization of the radiosynthesis of the Alzheimer tracer 2-(4-N-[11C]methylaminophenyl)-6-hydroxybenzothiazole ([11C]PIB).

Abstract
[(11)C]PIB is still the standard PET compound for Alzheimer imaging targeting beta-amyloid plaques. We aimed to establish a fully-automated procedure for the synthesis and purification of [(11)C]PIB with a high degree of reliability and improved specific activity as well as a suitable and fast quality control assay. The optimum reaction conditions were 75°C, 4 mg/mL precursor yielding at 48.0±2.7% (EOS, based on [(11)C]CH(3)OTf, corrected for decay), 183±14 GBq/μmol specific activity and >99% radiochemical purity. Time consumption was kept to a minimum (40 min from EOB) and overall yields were enough to serve 2 consecutive patients with a single preparation.
AuthorsC Philippe, D Haeusler, M Mitterhauser, J Ungersboeck, H Viernstein, R Dudczak, W Wadsak
JournalApplied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine (Appl Radiat Isot) Vol. 69 Issue 9 Pg. 1212-7 (Sep 2011) ISSN: 1872-9800 [Electronic] England
PMID21550258 (Publication Type: Journal Article)
CopyrightCopyright © 2011 Elsevier Ltd. All rights reserved.
Chemical References
  • 2-(4'-(methylamino)phenyl)-6-hydroxybenzothiazole
  • Aniline Compounds
  • Benzothiazoles
  • Carbon Radioisotopes
  • Radiopharmaceuticals
  • Thiazoles
Topics
  • Alzheimer Disease (diagnostic imaging)
  • Aniline Compounds
  • Automation, Laboratory (methods)
  • Benzothiazoles (chemical synthesis)
  • Carbon Radioisotopes
  • Humans
  • Isotope Labeling (methods)
  • Plaque, Amyloid (diagnosis, pathology)
  • Radionuclide Imaging
  • Radiopharmaceuticals (chemical synthesis)
  • Thiazoles

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