6-Fluoro-7-pyridylquinolone carboxylic esters and acids having antibacterial activity are prepared by coupling of a 2-fluorophenyl-metallic compound with a pyridyl bromide or iodide in the presence of a transition metal catalyst, nitrating and hydrogenating the pyridyl-2-fluorophenyl compound formed, introducing a substituent on the nitrogen of the amine formed, and cyclizing after reacting with a dialkyl or dibenzyl ethoxymethylene malonate to form a 6-fluoro-7-pyridyl-1,4-dihydroquinol-4-one 3-carboxylate, and hydrolyzing to the corresponding acid.
通过在转移
金属催化剂存在下将2-
氟苯基
金属化合物与
吡啶溴化物或
碘化物偶联,硝化和氢化所形成的
吡啶-2-
氟苯基化合物,引入胺基氮上的取代基,与二烷基或二苄乙氧亚
甲基丙二酸酯反应后环化形成6-
氟-7-
吡啶基-1,4-二氢
喹啉-4-酮-3-
羧酸酯,并
水解成相应的酸,制备具有抗菌活性的6-
氟-7-
吡啶基
喹诺酮羧酯和酸。