4.1 Article

Automated radiosynthesis of the Pittsburg compound-B using a commercial synthesizer

Journal

NUCLEAR MEDICINE COMMUNICATIONS
Volume 29, Issue 10, Pages 920-926

Publisher

LIPPINCOTT WILLIAMS & WILKINS
DOI: 10.1097/MNM.0b013e328304e0e1

Keywords

Alzheimer; automated synthesis; (11)C-labelled Pittsburgh compound-B; [(11)C]methyl triflate; positron emission tomography

Funding

  1. Advanced Accelerator Applications (France)

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Background The Pittsburgh compound-B ([(11)C]PIB) is a highly interesting radiotracer for imaging amyloid plaques in Alzheimer's disease by positron emission tomography (PET). An increasing number of PET centres schedule its transfer for clinical studies and therefore are interested in its automated synthesis. Method With the aim of flexibility, we reported the first fully automated synthesis of [(11)C]PIB with the coupling of two commercial synthesizers. Results [(11)C]PIB was prepared from 2-(4'-aminophenyl)-6-hydroxybenzothiazole by [(11)C]methyl triflate methylation reacting in an high-performance liquid chromatography loop and resulting in a total radiochemical yield of 13 +/- 15% after a synthesis time of 25 min. The specific activity of [(11)C]PIB was 20-60 GBq/mu mol and its radiochemical purity is more than 99%. Conclusion The rapid synthesis and the automatic auto-cleaning procedure allow convenient and reproducible [(11)C]PIB synthesis to be performed during the same day for preclinical or clinical PET scans.

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