Cheguillaume, Arnaud
Gillart, Jacques
[UCL]
Labar, Daniel
[UCL]
Grégoire, Vincent
[UCL]
Marchand-Brynaert, Jacqueline
[UCL]
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.
Bibliographic reference |
Cheguillaume, Arnaud ; Gillart, Jacques ; Labar, Daniel ; Grégoire, Vincent ; Marchand-Brynaert, Jacqueline. Perfluorinated markers for hypoxia detection: synthesis of sulfur-containing precursors and [18F]-labelling.. In: Bioorganic & medicinal chemistry, Vol. 13, no. 4, p. 1357-67 (2005) |
Permanent URL |
http://hdl.handle.net/2078.1/10084 |