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

Author(s): János Marton*, Attila Sipos, Sándor Berényi, Brita Glaenzel, Gjermund Henriksen*

Journal Name: Letters in Organic Chemistry

Volume 17 , Issue 11 , 2020

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Graphical 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.

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Article Details

Year: 2020
Published on: 29 November, 2020
Page: [845 - 856]
Pages: 12
DOI: 10.2174/1570178616666190905144136
Price: $65

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