title: 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.
authors.affiliation: Department of Nuclear Medicine, Medical University of Vienna, Radiochemistry and Biomarker Development Unit, Austria.
authors.forename: C
authors.initials: C
authors.lastname: Philippe
authors.forename: D
authors.initials: D
authors.lastname: Haeusler
authors.forename: M
authors.initials: M
authors.lastname: Mitterhauser
authors.forename: J
authors.initials: J
authors.lastname: Ungersboeck
authors.forename: H
authors.initials: H
authors.lastname: Viernstein
authors.forename: R
authors.initials: R
authors.lastname: Dudczak
authors.forename: W
authors.initials: W
authors.lastname: Wadsak
mesh_terms: D000544:Alzheimer Disease / Q000000981:diagnostic imaging; D000814:Aniline Compounds; D057205:Automation, Laboratory / Q000379:methods; D052160:Benzothiazoles / Q000138:chemical synthesis*; D002250:Carbon Radioisotopes; D006801:Humans; D007553:Isotope Labeling / Q000379:methods*; D058225:Plaque, Amyloid / Q000175:diagnosis / Q000473:pathology; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D013844:Thiazoles
chemical_list: C475519:2-(4'-(methylamino)phenyl)-6-hydroxybenzothiazole; D000814:Aniline Compounds; D052160:Benzothiazoles; D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; D013844:Thiazoles