期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 13, 期 4, 页码 1357-1367出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2004.11.010
关键词
hypoxia detection; [F-18]-labelling; trithioorthoester; alpha,alpha '-difluorodithioester
Syntbetic pathways of two novel sulfurated precursors for [F-18]-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 [F-18]-3,3,3-trifluoropropylamine, a convenient radiolabelled intermediate for [F-18]-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 [F-18]-radiochemistry are also presented. (C) 2004 Elsevier Ltd. All rights reserved.
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