2‐Nitroimidazole Based PET Tracers: Development of a General Synthetic Approach and Fluorination Methodology

Abstract

2-Nitroimidazole based PET tracers are widely used for noninvasive 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).