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Letters in Organic Chemistry

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ISSN (Print): 1570-1786
ISSN (Online): 1875-6255

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Research Article

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

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

Volume 17, Issue 11, 2020

Page: [845 - 856] Pages: 12

DOI: 10.2174/1570178616666190905144136

Price: $65

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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