| 摘要 |
The invention relates to a process for the preparation of antibacterial quinoline-3-carboxylic acids at the 7 position substituted with α amino acid of the formula [see Swedish original for formula] wherein X is CH, CF, CC1, CCF3, COR2 or CNR2R3, Y is H, F, NH2 or OR2, Z is [see Swedish original for formula] R is H, C1-6 alkyl or a cation, R1 is C1-6 alkyl, haloalkyl, wherein the alkyl has 1-4 carbon atoms, vinyl, C3-6 cycloalkyl, aryl or aryl substituted with halogen, hydroxy, amino or C1-4 alkyl, R2 and R3 are each independently hydrogen or C1-4 alkyl, R4 is -(CR2R3)n- NR2R5, wherein n is 0, 1 or 2, R5 is -C(=0)-CH(NH2)-R6, wherein R6 is hydrogen, C1-10 alkyl, C1-10 alkyl substituted with OR2, NR2R3, CO2H, CO2R2, CONR2R3, -CN(=NH)R2R3, SR2, SS-CH2-CH(NH2)-CO2H, CN, aryl or aryl substituted with halogen, hydroxy, amino or C1-4 alkyl, or it is phenyl, p-hydroxyphenyl or when taken together with nitrogen atom of a α amino group trimethylene or trimethylene substituted with hydroxy, for the preparation of optically active isomers or pharmaceutically accepted acid addition salts thereof.
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