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

C Philippe; D Haeusler; M Mitterhauser; J Ungersboeck; H Viernstein; R Dudczak; W Wadsak

doi:10.1016/j.apradiso.2011.04.010

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

Appl Radiat Isot. 2011 Sep;69(9):1212-7. doi: 10.1016/j.apradiso.2011.04.010. Epub 2011 Apr 29.

Authors

C Philippe¹, D Haeusler, M Mitterhauser, J Ungersboeck, H Viernstein, R Dudczak, W Wadsak

Affiliation

¹ Department of Nuclear Medicine, Medical University of Vienna, Radiochemistry and Biomarker Development Unit, Austria.

PMID: 21550258
DOI: 10.1016/j.apradiso.2011.04.010

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.

MeSH terms

Alzheimer Disease / diagnostic imaging
Aniline Compounds
Automation, Laboratory / methods
Benzothiazoles / chemical synthesis*
Carbon Radioisotopes
Humans
Isotope Labeling / methods*
Plaque, Amyloid / diagnosis
Plaque, Amyloid / pathology
Radionuclide Imaging
Radiopharmaceuticals / chemical synthesis*
Thiazoles

Substances

2-(4'-(methylamino)phenyl)-6-hydroxybenzothiazole
Aniline Compounds
Benzothiazoles
Carbon Radioisotopes
Radiopharmaceuticals
Thiazoles