C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/294.2, 260/2
C07D 213/80 (2006.01) C07D 211/90 (2006.01) C07D 401/02 (2006.01)
Patent
CA 1110234
ABSTRACT This invention is concerned with a process for the preparation of 4-pyridone-3-carboxylic acid derivatives of the general formula Image (I) wherein R1 represents a C1-8-alkyl, C3-10- -cycloalkyl, C3-10-cycloalkyl- -C1-6-alkyl, C1-6-alkoxy or C1-6-alkoxy-C1-6-alkyl group; R2 represents a hydrogen atom or a C1-6-alkyl group; R3 represents a phenyl, phenethyl or styryl group, which is optionally substituted by R4, R5 and/or R6, or an aromatic heterocyclic 6- -membered ring containing one or more N-atoms, which is linked via a ring C-atom and which is optionally substituted by R7; R4 and R5 each represent a halogen atom or a trifluoromethyl, hydroxy, C1-6-alkoxy, C1-6-alkylthio, C1-6- -alkyl, amino, acylamino, C1-6- -alkylamino, di-C1-6-alkylamlno or nitro group or a 5-membered or 6- -membered heterocycle linked via a ring N- or C-atom or R and R5 together represent a C1-6-alkylene- dioxy group; R6 represents a C1-6-alkoxy group and R7 represents a halogen atom or a hydroxy, C1-6-alkoxy, C1-6-alkyl- thio, C1-6-alkyl, amino, C1-6- -alkylamino or di-C1-6-alkylamino groups with the proviso that R2 represents a C1-6-alkyl group when R1 represents the methyl group and simultaneously R3 represents the phenyl group, and of salts thereof, which process comprises (a) dehydrogenating a 1,4,5,6-tetrahydronicotinic acid derivative of the general formula Image (II) , wherein R1, R and R3 are defined as above, in the 5,6-position, or (b) modifying a substituent R2 and/or R3 in a manner known per se within the definitions given above, and, if desired, converting the compound of formula I obtained into a salt and with pharmaceutical preparations con- taining same. These derivatives possess antibacterial activity and/or a stimulating activity on the central nervous system.
318702
Gowling Lafleur Henderson Llp
Hoffmann-La Roche Limited
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