摘要
氧氟沙星由2,3,4一三氟硝基苯经选择性碱水解、醚化、还原、缩合环合蝥合、缩舍与水解等五步制得,步骤短,反应条件温和,副反应少,总收率30％以上,较文献收率高8～15％。
An improved synthesis of antibacterial agent ofloxacin wasdescribed.Alkaline hydrolysis of 2,3,4-trifluoronitrobenzene(2)gave o-nitrophenol derivative(3).The 2-acetonyloxy compound(4)was converted tobenzoxazine derivative(5)by reductive cyclization.Condensation,cyclization andchelation of 5 with EMME and B(OAc)_3 successively afforded 6,which,in turn,was condensed with 4-methylpiperazine followed by hydrolysis to give ofloxacin(1).The overall yield was over 30%.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
1991年第9期385-387,共3页
Chinese Journal of Pharmaceuticals
关键词
氧氟沙星
氟喹诺酮类
抗菌剂
合成
ofloxacin
fluoroquinolone antimicrobial agent
synthesis
