发明名称 NOVEL PRECURSOR MOLECULES FOR LABELLED F-18 PET RADIOACTIVE INDICATORS
摘要 FIELD: chemistry.SUBSTANCE: invention relates to novel compounds of general formula II in form of stereoisomeric forms and suitable salts with organic or inorganic acid, as well as to method of obtaining thereof. Invention also relates to synthesis of formula If compounds with application of said formula II precursors. Formula If compounds can be used as radioactive PET indicators for molecular diagnostics of various diseases in field of oncology, neurology, and cardiology. In general formulas IIand Ifrepresents -C(U)(U)-C?CH, Uand Urepresents hydrogen; A represents phenyl, Ris selected from (C-C)-alkyl, Ris substitutable group, selected from halogen and (C-C)alkylsulphonyloxy. Method of obtaining formula II compound includes reaction of compound of formula Ia, where W, A and Rhave said values with suitable reagents to achieve transformation of hydroxyl group of formula Ia into substitutable group R. Reaction mixture is exposed at low temperature and then heated to temperature between 70°C-130°C. Method of synthesis of formula If compound includes reaction of formula IIcompound, where W, A, Rand Rhave values given above, with F-fluorinating agent, in which F=F, with heating of reaction mixture to temperature between 70°C-130°C. Invention also relates to set for preparation of If compounds, which contains hermetic ampoule, containing compound, selected from formula II compounds.EFFECT: formula II compounds can be used as precursors for preparation of certain labelledF radioactive indicators of positron-emission tomography (PET).13 cl, 11 dwg, 3 ex
申请公布号 RU2538276(C2) 申请公布日期 2015.01.10
申请号 RU20110147110 申请日期 2010.04.10
申请人 PIRAMAL IMEHDZHING SA 发明人 GEORG KETCHAU;TOBIAS GENRIKH;LUTTS LEMANN;SHTEFAN ZIGEL';SANGRAM NAG
分类号 C07C209/74;C07C211/29;C07C309/66 主分类号 C07C209/74
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