| 摘要 |
<p>Novel racemates or optically active forms of 2-amino-4-hydroxy-3-quinoline carboxylic acid derivatives of the formula <IMAGE> I wherein X is in the 5-, 6-, 7- or 8-position and is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 4 carbon atoms, CF3-, CF3S- and CF3O-, R1 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R2 is selected from the group consisting of (a) thiazolyl, 4,5-dihydrothiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidyl and tetrazolyl, each optionally substituted with alkyl of 1 to 4 carbon atoms and (b) phenyl optionally substituted with at least one member of the group consisting of hydroxy, alkyl and alkoxy of 1 to 4 carbon atoms, CF3-, -NO2 and halogen, R3 is selected from the group consisting of 2-pyrrolidinyl of the formula <IMAGE> R4 is selected from the group consisting of hydrogen, an amino protective group and <IMAGE> R'4 is selected from the group consisting of alkyl 1 to 5 carbon atoms optionally substituted with amino or protected amino, aryl and aralkyl, R5 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, aryl, aralkyl, p-hydroxy-benzyl, lH-indol-3-yl methyl of the formula <IMAGE> and -CH2SH, the last three being optionally protected by a blocking group and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic and anti-inflammatory activity and novel intermediates.</p> |
