Perfluorinated markers for hypoxia detection: synthesis of sulfur-containing precursors and [18F]-labelling |
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Authors: | Cheguillaume Arnaud Gillart Jacques Labar Daniel Grégoire Vincent Marchand-Brynaert Jacqueline |
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Affiliation: | Unité de Chimie Organique et Médicinale, Batiment Lavoisier, place L. Pasteur, Université catholique de Louvain, B-1348 Louvain-la-Neuve, Belgium. |
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Abstract: | Synthetic pathways of two novel sulfurated precursors for [18F]-labelling by oxidative fluorodesulfurization reaction are described. A three-step sequence starting from N-phthalimido-beta-alanine allows the preparation of a new trithioorthoester as valuable precursor of the synthesis of [18F]-3,3,3-trifluoropropylamine, a convenient radiolabelled intermediate for [18F]-EF3. A five-step sequence for the preparation of methyl 4-phthalimido-2,2-difluoropropanedithioate from ethyl 2,2-difluoropropanoate, via the key conversion step of alpha,alpha'-difluorothioamidate to the corresponding alpha,alpha'-difluorodithioester, and the first results of its use as precursor for oxidative fluorodesulfurization in [18F]-radiochemistry are also presented. |
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