2-Nitroimidazole Based PET Tracers: Development of a General Synthetic Approach and Fluorination Methodology |
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| Authors: | Dr Kévin Renault Romain Horion Xavier Maes Maha Rzeigui Dr Yoann Joyard Dr Nicolas Maindron Dr Vincent Tadino Prof Stéphane Vincent |
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| Institution: | 1. Département de Chimie, Laboratoire de Chimie Bio-Organique, University of Namur (FUNDP), Rue de Bruxelles 61, 5000 Namur, Belgium;2. ORA-Neptis, Rue de la Salette 15, 5600 Neuville, Belgium |
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| Abstract: | 2-Nitroimidazole based PET tracers are widely used for non-invasive hypoxic tumor diagnosis. In this context, we report here a general method based on a central Mitsunobu reaction to easily access 2-nitroimidazole precursors. Optimization of fluorination conditions is described and successfully applied to the radiofluorination of the 2-nitroimidazole precursors. Moreover, the radiosynthesis of a new potential hypoxia PET tracer is also described. Finally, this article presents a SFC analytical method allowing both an easy monitoring of the fluorination reactions and the measurement of partition coefficients (logP). |
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| Keywords: | fluorination Mitsunobu reaction PET tracer synthetic methods hypoxia |
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