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Synthesis of 1,1′ [11C]-methylene-di-(2-naphthol) ([11C]ST1859) for PET studies in humans

✍ Scribed by Oliver Langer; Andreas Krcal; Alexander Schmid; Aiman Abrahim; Patrizia Minetti; Diana Celona; Dirk Roeda; Frédéric Dollé; Kurt Kletter; Markus Müller

Publisher
John Wiley and Sons
Year
2005
Tongue
French
Weight
170 KB
Volume
48
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

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 [^11^C]formaldehyde with 2‐naphthol. [^11^C]formaldehyde was prepared by catalytic dehydrogenation of [^11^C]methanol (conversion yield: 48±11% (n = 19)) employing a recently developed silver‐containing ceramic catalyst. Starting from 69±3 GBq of [^11^C]carbon dioxide (n = 19), 4±1 GBq of [^11^C]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 [^11^C]ST1859 at the end of synthesis exceeded 32 GBq/µmol. Copyright © 2005 John Wiley & Sons, Ltd.

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