Design and Synthesis of an 18F-Labeled Version of Phenylethyl Orvinol 18FFE-PEO for PET-Imaging of Opioid ReceptorsReportar como inadecuado




Design and Synthesis of an 18F-Labeled Version of Phenylethyl Orvinol 18FFE-PEO for PET-Imaging of Opioid Receptors - Descarga este documento en PDF. Documentación en PDF para descargar gratis. Disponible también para leer online.

1

ABX Advanced Biochemical Compounds Biomedizinische Forschungsreagenzien GmbH, Heinrich-Glaeser-Strasse 10-14, D-01454 Radeberg, Germany

2

Oslo PET-Centre, Norsk Medisinsk Syklotronsenter AS, N-0027 Oslo, Norway

3

Institute of Basic Medical Sciences, Group of Pharmaceutical Radiochemistry, University of Oslo, Postboks 1110 Blindern, N-0317 Oslo, Norway





*

Author to whom correspondence should be addressed.



Abstract The semisynthetic oripavine derivative phenethyl orvinol PEO, a full agonist at opioid receptors OR, is an attractive structural motif for developing 18F-labeled PET tracers with a high degree of sensitivity for competition between endogenous and exogenous OR-ligands. The target cold reference compound 6-O-2-fluoroethyl-6-O-desmethylphenylethyl orvinol FE-PEO was obtained via two separate reaction routes. A three-step synthesis was developed for the preparation of a tosyloxyethyl precursor TE-TDPEO, the key precursor for a direct, nucleophilic radiofluorination to yield 18FFE-PEO. The developed radiosynthesis provides the target compound in relevantly high yield and purity, and is adaptable to routine production. View Full-Text

Keywords: opioid receptors; PET; agonist; 18F-fluorination; automated radiosynthesis opioid receptors; PET; agonist; 18F-fluorination; automated radiosynthesis





Autor: János Marton 1 and Gjermund Henriksen 2,3,*

Fuente: http://mdpi.com/



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