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Preparation of 4-[11C]methylmetaraminol, a potential PET tracer for assessment of myocardial sympathetic innervation

✍ Scribed by Oliver Langer; Tobias Forngren; Johan Sandell; Frédéric Dollé; Bengt Långström; Kjell Någren; Christer Halldin

Publisher
John Wiley and Sons
Year
2002
Tongue
French
Weight
114 KB
Volume
46
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

The false adrenergic neurotransmitter [^11^C]meta‐hydroxyephedrine ([^11^C]HED) is currently the PET tracer of choice for assessment of myocardial sympathetic innervation. The molecule is metabolised in the 4‐position of the aromatic ring. The resulting radiolabelled metabolites need to be measured in order to obtain an arterial input function. Our aim was the development of a PET tracer with an increased metabolic stability relative to [^11^C]HED. We selected 4‐methylmetaraminol as a candidate molecule for radiolabelling with ^11^C (t~1/2~ 20.4 min). Our radiosynthetic approach towards 4‐[^11^C]methylmetaraminol involved a palladium‐catalyzed cross‐coupling reaction of a protected 4‐trimethylstannyl derivative of metaraminol with [^11^C]methyl iodide followed by removal of the protective groups. 4‐[^11^C]methylmetaraminol was obtained in a final decay‐corrected radiochemical yield of 20–25% within a synthesis time of 60–80 min. The specific radioactivity at the end of the synthesis ranged from 18–37 to GBq/μmol. The unlabelled reference molecule, 4‐methylmetaraminol, was prepared in a 5‐step synthesis starting from metaraminol. A biological evaluation of 4‐[^11^C]methylmetaraminol is in progress and the results will be reported elsewhere. Copyright © 2002 John Wiley & Sons, Ltd.

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