| Autor: |
Langer, Oliver, Krcal, Andreas, Schmid, Alexander, Abrahim, Aiman, Minetti, Patrizia, Celona, Diana, Roeda, Dirk, Dollé, Frédéric, Kletter, Kurt, Müller, Markus |
| Zdroj: |
Journal of Labelled Compounds and Radiopharmaceuticals; July 2005, Vol. 48 Issue: 8 p577-587, 11p |
| Abstrakt: |
1,1′‐Methylene‐di‐(2‐naphthol) (ST1859), a candidate drug for the treatment of Alzheimer's disease, was radiolabelled with carbon‐11 with the aim to perform PET microdosing studies in humans. The radiosynthesis was automated in a commercial synthesis module (Nuclear Interface PET tracer synthesizer) and proceeded via reaction of [11C]formaldehyde with 2‐naphthol. [11C]formaldehyde was prepared by catalytic dehydrogenation of [11C]methanol (conversion yield: 48±11% (n = 19)) employing a recently developed silver‐containing ceramic catalyst. Starting from 69±3 GBq of [11C]carbon dioxide (n = 19), 4±1 GBq of [11C]ST1859 (decay‐corrected to the end of bombardment), readily formulated for intravenous administration, could be obtained in an average synthesis time of 38 min. The specific radioactivity of [11C]ST1859 at the end of synthesis exceeded 32 GBq/µmol. Copyright © 2005 John Wiley & Sons, Ltd. |
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