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A New Precursor for the Radiosynthesis of 6-O-(2-[18F]Fluoroethyl)-6-Odesmethyl- diprenorphine ([18F]FE-DPN) by Nucleophilic Radiofluorination

[ Vol. 18 , Issue. 5 ]

Author(s):

János Marton*, Paul Cumming, Beate Bauer and Gjermund Henriksen*   Pages 344 - 352 ( 9 )

Abstract:


We present the preparation of the new precursor 6-O-(2-tosyloxyethoxy)-6-O-desmethyl-3- O-trityl-diprenorphine (TE-TDDPN) for a one-pot, two-step nucleophilic radiosynthesis of 6-O-(2- [18F]fluoroethyl-6-O-desmethyl-diprenorphine ([18F]FE-DPN). The route to the precursor consists of a five-step synthesis starting from diprenorphine. We also provide alternative synthesis routes for the cold reference standard and the complete 1H- and 13C-NMR assignment of the prepared derivatives.

Keywords:

Fluoroethyl-diprenorphine, opioid receptors, positron emission tomography, orvinols, PET-precursor, 6, 14- ethenomorphinans.

Affiliation:

ABX Advanced Biochemical Compounds Biomedizinische Forschungsreagenzien GmbH, Heinrich-Glaeser-Strasse 10- 14, D-01454 Radeberg, Department of Nuclear Medicine, University of Bern, Inselspital, Freiburgstraße 18, 3010 Bern, ABX Advanced Biochemical Compounds Biomedizinische Forschungsreagenzien GmbH, Heinrich-Glaeser-Strasse 10- 14, D-01454 Radeberg, Institute of Basic Medical Sciences, University of Oslo, P. O. Box 1105, Blindern, N-0317 Oslo

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