FIELD: veterinary medicine.
SUBSTANCE: invention relates to a method for obtaining a compound of formula (1) in the form of a mixture of diastereomers, which can be used for the treatment of bacterial infections in animals. The method includes stages a)-d). At stage a), the compound of formula (B) is pre-activated on a palladium catalyst in the presence of alcohol, a ligand selected from a group consisting of 2-dicyclohexylphosphino-2',4',6'- triisopropylbiphenyl, 2-dicyclohexylphosphino-2,6-dimethoxybiphenyl, 1,3-bis(diphenylphosphino)propane, ferrocenediyl bis(diphenylphosphine), dibenzylidenacetone, triphenylphosphine and tricyclohexylphosphine, and a buffer for borylation, which contains an acid and a base, and this acid is selected from a group consisting of acetic acid, citric acid, formic acid and chloroacetic acid, and the base is selected from a group consisting of potassium acetate, caesium acetate, triethylamine, potassium carbonate, sodium carbonate, caesium carbonate, diisopropylethylamine and potassium tribasic phosphate and their mixtures. At stage b), the pre-activated compound of formula (B) is borylated from stage a) by adding a borylating agent in alcohol, and the borylating agent is selected from a group consisting of bisboronic acid, bisboronic acid and ethylene glycol, bisboronic acid and propylene glycol, bis(pinacolato)dibora and tetrakis(dimethylamino)dibora. At stage c), the compound of formula (A) is mixed with the base of the buffer for borylation in alcohol, a solvent or with mixtures thereof, and at stage d) reagents from stage c) are added to reagents from stage b) to obtain a compound of formula (1). The invention also relates to a variant of this method.
EFFECT: proposed method includes fewer chemical stages and provides a higher yield.
12 cl, 3 dwg, 4 tbl
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