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4-Anilidopiperidine Derivatives for in vivo Imaging of μ-Opioid Receptors

[ Vol. 17 , Issue. 11 ]

Author(s):

János Marton*, Attila Sipos, Sándor Berényi, Brita Glaenzel and Gjermund Henriksen*   Pages 845 - 856 ( 12 )

Abstract:


A method for gram scale preparation of 2-fluoropropionyl-carfentanil was established, starting from 4-phenylamino-1-benzyl-4-piperidinecarboxylic acid. 2-Fluoropropionyl-carfentanil carboxylic acid and 2-chloropropionyl-carfentanil as precursors were synthesized for the radiosynthesis of 11C and/or 18F labelled 2-fluoropropionyl-carfentanil derivatives via two separate reaction routes. Conformational analysis of 2-fluoropropionyl-carfentanil was performed using computational methods. Calculated 1H and 13C-NMR shifts are presented.

Keywords:

4-anilidopiperidines, 2-fluoropropionyl-carfentanil, 2-chloropropionyl-carfentanil, positron emission tomography, conformational analysis.

Affiliation:

ABX Advanced Biochemical Compounds Biomedizinische Forschungsreagenzien GmbH, Heinrich-Glaeser-Strasse 10-14, D-01454 Radeberg, Department of Pharmacological Chemistry, University of Debrecen, Health and Medical Center, PO Box 70, H-4010 Debrecen, Department of Organic Chemistry, University of Debrecen, PO Box 20, H-4010 Debrecen, 1ABX Advanced Biochemical Compounds Biomedizinische Forschungsreagenzien GmbH, Heinrich-Glaeser-Strasse 10-14, D-01454 Radeberg,, Institute of Basic Medical Sciences, University of Oslo, PO Box 1105, Blindern, N-0317 Oslo



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