| 摘要 |
<p>1374463 Substituted quinoline-3-carboxylic acids E R SQUIBB & SONS Inc 16 Sept 1971 [18 Sept 1970] 43280/71 Heading C2C [Also in Division A5] The invention comprises compounds of formula and their pharmaceutically acceptable salts, wherein Z is OH, C 1 -C 8 alkoxy, PhO or halogen; R 1 is H or C 1 -C 5 alkyl; R 2 is H, up to C 8 alkyl, alkoxy or alkenyl, C 3 -C 6 -ring cycloalkyl, Ph, CN, halogen, trihalomethyl or haloalkoxy; R 3 , R 4 , R 5 , R 6 are each H or C 1 -C 8 alkyl, or up to 2 of them may be Ph; R 7 is H, C 1 -C 8 alkyl or Ph; each Ph may be substituted and each alkyl or alkoxy may be substituted by Ph. These compounds are prepared by heating a dialkyl carboxyphenylaminomethylenemalonate at above 200‹ C., making the acid chloride of the 3-monoester of the appropriately substituted 4-hydroxyquinolinedicarboxylic acid so formed (the 4-OH group may be simultaneously converted to 4-halogen), and reacting this with the corresponding aziridine; the 4-alkoxy or aryloxy compounds may be made by reacting the 4-OH compounds with the appropriate halide or sulphate; and any of the ester products may be hydrolysed to the corresponding acids.</p> |
