FIELD: chemical industry.
SUBSTANCE: method for the hydrolysis of esters of quinolone carboxylic acids of general formula (II) to obtain quinolone carboxylic acids of general formula (I):
where, respectively, in formulas (I) and (II): R2 is hydrogen, methyl, methoxy, fluorine, chlorine, nitro or cyano, R3 is fluorine or chlorine, R4 is fluorine, R5 is hydrogen, methyl, fluorine, chlorine or nitro and Υ is methyl, ethyl, isopropyl, cyclopropyl, fluorocyclopropyl, 4-fluorophenyl or 2,4-difluorophenyl, and in formula (I) R1 is methyl or ethyl, which includes the step: A) reacting compounds of formula (II) with a mixture containing acetic acid, sulfuric acid and water, which differs in that in step A) from 30 to 40 mol of acetic acid, from 0.3 to 1 mol of sulfuric acid and from 0.9 up to 2.5 mol of water is used in terms of mol of compounds of formula (II).
EFFECT: improved method of hydrolysis of esters of quinolonecarboxylic acids of general formula (II) with the production of quinolonecarboxylic acids of general formula (I), in which the formation of by-products to be processed is as small as possible and in which the resulting quinolonecarboxylic acid has the highest possible purity.
8 cl, 1 dwg
| Title |
Year |
Author |
Number |
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