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Mise au point de nouvelles techniques de radio-iodation et application au radiomarquage de molécules d'intérêt

Abstract : Labeling of (bio)molecules with radioactive isotopes is of high interest to for the scientific commu-nity, as it strongly impacts the discovery process in life science and nuclear medicine. Radiolabeled molecules have been extensively used to assess biochemical reactions, to measure in vivo distribution of a substance or to preform RIA (RadioImmunoAssay). In nuclear medicine, radio-therapeutics for RIT (RadioIsotope Therapy) and radio-tracers for molecular imaging experiments such as PET (Positron Emission Tomography), SPECT (Single Photon Emission Computed Tomography) or scintigraphy have been described. Several useful isotopes of iodine can be used for both diagnosis and therapy: 123I for SPECT imaging, 124I for PET imaging, 125I for biological assays and 131I for radio-therapy and scintig-raphy.Classical methods of radioiodination methods use a prefunctionalized precursor, which must be syn-thesized, isolated and purified before being introduced to the radio-iodination step. The radioiodode-stannylation method is the most popular method, although stannylated precursors are known for their difficult synthesis and their toxicity. The development of new methods of radioiodination is therefore of great interest in the field of radiochemistry.Based on a previous work, our group has developed a method to radio-iodinate N-acylsulfonamides through a room temperature palladium mediated C-H radio-iodination. This original strategy allows radiolabeling of biomolecules in very mild conditions without the use of chemical precursors.Based on literature, our group is now developping a new method to radio-iodinate arylsilyl derivates through radioiododesilylation in mild conditions. This general methodology allows for the moment the radiolabeling of activated arylsilyl derivates in mild conditions.
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  • HAL Id : tel-02421209, version 1

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Alexandra Hebert. Mise au point de nouvelles techniques de radio-iodation et application au radiomarquage de molécules d'intérêt. Médecine humaine et pathologie. Normandie Université, 2019. Français. ⟨NNT : 2019NORMC413⟩. ⟨tel-02421209⟩

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