METHOD OF FLUORINATING ANILIDE DERIVATIVES AND FLUORINATED BENZOTHIAZOLE DERIVATIVES AS IN VIVO IMAGING AGENTS Russian patent published in 2011 - IPC C07C209/62 C07D277/66 C07B59/00 

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, C_1-6alkyl, C_1-6alkoxy, halogen, OCH₂OR¹¹, where R¹¹ is C_1-6alkyl; R¹ is C_1-6alkyl. 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, C_1-10alkyl, C_1-10halogenalkyl, -(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