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Nouvelles approches de marquage au fluor 18 et développement d'un radiotraceur pour l'imagerie TEP en oncologie

Abstract : PET is a medical imaging technique that uses positron-emitting radioactive atoms. One of the most common isotope used for PET imaging isfluorine-18, but the low reactivity of [¹⁸F]fluoride anion is still associated with labelling issues of some specific compounds. The introduction of fluorine on a non-activated aromatic ring remains a radiosynthesis challenge, limiting the development of radiotracers involving such scaffold. The first part of this work deals with the development of new strategies of radiofluorination using boron,known to have a high affinity with fluorine. Two approaches have been studied. The first one is based on the use of a boron atom to guide aromatic fluorination through a concerted nucleophilic aromatic substitution. The second one was the use of the fluorophilic borylated compounds aiming to tranfer aqueous [¹⁸F]fluorides anions produced in the cyclotron to an organic solvent to eliminate drying steps of the [¹⁸F]fluorides usually required. The second part of this work describes the radiolabeling of binimetinib, a drug prescribed for the treatment of BRAF mutant melanomas. Binimetinib is an inhibitor of the MAPK enzyme carrying two fluorine atoms. Beyond the challenge of [¹⁸F]binimetinib synthesis, this compound could be a key for the stratification of patients suffering from cancers involving specific mutations deregulating the RAS signalling pathway involved in cell survival and proliferation mechanism.
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Submitted on : Friday, June 11, 2021 - 1:01:09 AM
Last modification on : Monday, June 21, 2021 - 3:24:55 PM

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Rémi Pelletier. Nouvelles approches de marquage au fluor 18 et développement d'un radiotraceur pour l'imagerie TEP en oncologie. Chimie organique. Université Paris-Saclay, 2020. Français. ⟨NNT : 2020UPASF035⟩. ⟨tel-03257451⟩

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