NOVEL PRECURSOR MOLECULES FOR LABELLED F-18 PET RADIOACTIVE INDICATORS Russian patent published in 2015 - IPC C07C209/74 C07C211/29 C07C309/66 

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 II and If represents -C(U¹)(U²)-C≡CH, U¹ and U² represents hydrogen; A represents phenyl, R¹ is selected from (C₁-C₆)-alkyl, R² is substitutable group, selected from halogen and (C₁-C₃)alkylsulphonyloxy. Method of obtaining formula II compound includes reaction of compound of formula Ia , where W, A and R¹ have said values with suitable reagents to achieve transformation of hydroxyl group of formula Ia into substitutable group R². 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 II compound, where W, A, R¹ and R² have values given above, with F-fluorinating agent, in which F=¹⁸F, 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 labelled ¹⁸F radioactive indicators of positron-emission tomography (PET).

13 cl, 11 dwg, 3 ex