| 摘要 |
FIELD: chemistry. ^ SUBSTANCE: invention relates to a method of producing compounds of formula ^ , where the fluoro group is possibly [18F]fluoro; ring A is substituted with benzothiazol-2-yl, which is substituted with hydroxy, C1-6alkyl, C1-6alkoxy, halogen, OCH2OR11, where R11 is C1-6alkyl; R1 is C1-6alkyl. The method involves reaction of the corresponding compound of formula , where ring A is substituted as defined for the compound of formula (I); R2 is selected from hydrogen, C1-10alkyl, C1-10halogenalkyl, -(CH2CH2O)q-CH3, where q is an integer from 1 to 10; R1 is as defined for the compound of formula (I); R3 is a leaving group such as nitro, with an alkali metal fluoride or tetra-alkylammonium, possibly with [18F]fluoride, to obtain a compound of formula , where R1 and R2 are as defined for compounds of formulae (I) and (II), the fluoro group is possibly [18F]fluoro and ring A is substituted as defined for the compound of formula (I); with subsequent conversion of the -C(O)R2 group to hydrogen through hydrolysis and possible removal of any extra protective groups. The invention also relates to novel compounds of formulae ^ , where R1-R3, R9, defined above, are precursors of compounds of formula (I), as well as to a radiopharmaceutical set and a cartridge for use in positron emission tomography, which contain said precursors. ^ EFFECT: method enables to obtain compounds of formula (I) using a simpler and more efficient method. ^ 11 cl, 1 tbl, 6 ex |
