FIELD: organic chemistry, chemical technology. SUBSTANCE: invention relates to new derivatives of quinolone carboxylic acid of the formula (I) , their pharmaceutically acceptable salts and hydrates where X means hydrocarbon group, fluorocarbon group or nitrogen atom; Y means hydrogen atom or methyl group; R1 means hydrogen atom or C1-C5-alkyl group; R2 means a group of the formula (a) where A and B mean fluorocarbon group or nitrogen atom at condition that when A is CF then B is N and when A is N then B is CF; R3 means a group of the formula (b) where substitute R4 means amino-group with racemate or (S)-enantiomer formation, or a group of the formula (c) where substituents R5, R6 and R7 mean hydrogen atom or C1-C3-alkyl group. Derivative of quinolone carboxylic acid of the formula (I) is synthesized by condensation of compound of the formula (II) and compound of the formula HR3 in solvent in the presence of acid acceptor and excess of compound of the formula HR3 that is one of reagents. Solvent is taken from a group involving pyridine, acetonitrile, N,N-dimethylformamide. In compound of the formula (II) and compound of the formula HR3 substituents X, Y, Z, R1, R2 and R3 mean values indicated above. EFFECT: improved method of synthesis. 11 cl, 6 tbl, 29 ex
Authors
Dates
1998-10-27—Published
1994-01-21—Filed