METHOD OF PRODUCING SUBSTITUTED TETRAFLUOROBENZYL ANILINE COMPOUNDS AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF Russian patent published in 2011 - IPC C07C227/04 C07C227/14 C07C229/60 C07C229/64 C07C251/16 A61K31/196 A61P25/00 A61P25/28 

FIELD: chemistry.

SUBSTANCE: present invention relates to versions of the method of producing a derivative of tetrafluorobenzyl-5- aminosalicylic acid of formula I where R₁, R₂ and R₃ can independently denote hydrogen or halogen, which can be used to prevent or treat acute and chronic neurodegenerative diseases, particularly focal brain ischemia, and to a method of producing pharmaceutically acceptable salts of this derivative. One version of the method of producing the tetrafluorobenzyl-5-aminosalicylic acid derivative of formula I involves the following steps: a) oxidation of tetrafluorobenzyl alcohol of formula I to tetrafluorobenzaldehyde of formula 2 b) conversion of tetrafluorobenzaldehyde to a tetrafluorobenzylidine-5-aminosalicylic acid derivative of formula II through a dehydration-condensation reaction between tetrafluorobenzaldehyde and 5-aminosalicylic acid of formula 3 and c) hydrogenation of the tetrafluorobenzylidine-5-aminosalicylic acid derivative to a tetrafluorobenzyl-5-aminosalicylic acid derivative of formula I.

EFFECT: efficient method of producing tetrafluorobenzyl-5-aminosalicylic acid derivative.

4 cl, 9 tbl, 1 dwg, 11 ex