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Synthesis of 1,1′ [ 11 C]‐methylene‐di‐(2‐naphthol) ([ 11 C]ST1859) for PET studies in humans
Author(s) -
Langer Oliver,
Krcal Andreas,
Schmid Alexander,
Abrahim Aiman,
Minetti Patrizia,
Celona Diana,
Roeda Dirk,
Dollé Frédéric,
Kletter Kurt,
Müller Markus
Publication year - 2005
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.951
Subject(s) - radiosynthesis , chemistry , formaldehyde , methanol , methylene , catalysis , radiochemistry , nuclear chemistry , dehydrogenation , yield (engineering) , carbon 14 , chemical synthesis , medicinal chemistry , organic chemistry , nuclear medicine , medicine , biochemistry , materials science , metallurgy , in vitro , positron emission tomography , physics , quantum mechanics
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.