Norfloxacin And Its Derivatives 7 - Substituent Modification,

Quinolones Antibacterial Agents is a kind of effective and quickly developing pharmaceutical after 13 lactam.The study of its structural reformation is still active. Introducing unsymmetrical carbon atom or chiral group would reduce the toxic while increase the effect. This thesis aims at introducing chiral group to N-atom at quinolones?7-position piperazinyl through alkylation ( or acylation) reaction We did research works as follow: 1. Synthesis of Norfloxacin analogs from 3-chloro-4-floro aniline and 2,3,4-trifloro nitrobenzene. 2. In the synthesis of substituted quinolone's main cycle, we used Microwave Irradiation instead of traditional heating and got the target molecular conveniently, quickly and high-yielded. 3. During the Ethylation of 6-floro7-chloro quinolone, increasing of the reaction pressure resulted in lower source's ratio and shorter reaction time. 4. In the course of introducing chiral group to quinolone , PTC technology was used in the N-alkylation. This method is mediate, quick and high-yielded. 5. Ten quinolones?compounds with a chiral group were synthesized in total. Nine of them were new compounds. Six of them are optically active. All the synthesized compounds were characterized by c-NMR, JR and Elemental Analysis. Two of them have good solution in water. More pharmaceutical study would be done about them.