Novel synthesis of fluoroquinolones

摘要

Preparing fluoroquinolone compound of formula (I) or its hydrates and/or acid or base addition salts, comprises reacting substituted quinoline compound (II) with an amine compound (A1) in water, and optionally recovering the obtained compound (I). Preparing fluoroquinolone compound of formula (I) or its hydrates and/or acid or base addition salts, comprises reacting substituted quinoline compound of formula (II) with an amine compound of formula (R 3R 4NH) (A1) in water, and optionally recovering the obtained compound (I). R 1H, alkyl or NRR1a; R 2F; either R 3, R 4(cyclo)alkyl, aralkyl (optionally substituted by OH or NRR1a), H or OH; or NR 3R 4heterocycle (optionally substituted by alkyl, OH, alkoxy, -C(=O)alkyl, NRR1a, =NOR, aralkyl or (hetero)aryl, where the alkyl or (hetero)aryl groups is optionally substituted by alkyl, halo, perfluoroalkyl, alkoxy or NRR1a); R 5alkyl, aryl (optionally substituted by halo or OH), H, cycloalkyl, NR(CHO) or NRR1a; X : CR 8 or N; either R 8H, halo, alkyl or alkoxy; or R 8R 5heterocycle (optionally substituted by alkyl); R, R1a : H or alkyl; R 6halo; and R 7alkyl. [Image] ACTIVITY : Antibacterial. MECHANISM OF ACTION : Topoisomerase II inhibitor; DNA-gyrase inhibitor; DNA replication inhibitor; DNA transcription inhibitor.