[Tetrazoyl-11C]LY202157 synthesis for in vivo studies of the NMDA receptor channel complex

[Tetrazoyl‐11C]LY202157 8 was prepared via a three step synthesis from ethyl (3S,4aR,6S,8aR)‐6‐bromomethyl‐2‐methoxycarbonyl‐1,2,3,4,4a,5,6,7,8,8a‐decahydroisoquinoline‐3‐carboxylate 4. This bromo precursor was reacted with [11C]hydrogen cyanide affording the corresponding [11C]nitrile. Conversion t...

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Bibliographic Details
Published in:Journal of labelled compounds & radiopharmaceuticals 2000-11, Vol.43 (13), p.1311-1320
Main Authors: Ponchant, M., Galéa, H., Bottlaender, M., Coulon, C., Fuseau, C., Ottaviani, M., Crouzel, C.
Format: Article
Language:English
Subjects:
[11C]-1H-tetrazoyl
[11C]HCN
Biological and medical sciences
Contrast media. Radiopharmaceuticals
Medical sciences
NMDA receptor
PET ligand
Pharmacology. Drug treatments
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Summary:[Tetrazoyl‐11C]LY202157 8 was prepared via a three step synthesis from ethyl (3S,4aR,6S,8aR)‐6‐bromomethyl‐2‐methoxycarbonyl‐1,2,3,4,4a,5,6,7,8,8a‐decahydroisoquinoline‐3‐carboxylate 4. This bromo precursor was reacted with [11C]hydrogen cyanide affording the corresponding [11C]nitrile. Conversion to the tetrazole was achieved by treatment with azidotributyltin followed by hydrolysis with 6N hydrochloric acid at 200°C. After HPLC purification and analytical HPLC control, more than 370 MBq (10 mCi) of [tetrazoyl‐11C] LY202157 were obtained after an overall 60 minute synthesis time with 38% yield (EOB) and specific activity of 25.9 GBq/µmol (700 mCi/µmol). Ex vivo biological studies showed that the [tetrazoyl‐11C] LY202157 did not cross the brain blood barrier. Copyright © 2000 John Wiley & Sons, Ltd.
ISSN:0362-4803
1099-1344
DOI:10.1002/1099-1344(200011)43:13<1311::AID-JLCR422>3.0.CO;2-B