盐酸芦氟沙星合成工艺研究

Studies on Synthesis of a New Tricyclic Fluoroquinolone Rufloxacin Hydrochloride

设计了一条合成含硫三环氟喹诺酮抗菌药盐酸芦氟沙星（１）的新方法，总收率达３２．５％。以２，３，４－三氟硝基苯为起始原料，经取代、还原、溴化、环合、缩环、螯合、甲哌化、水解成盐等八步反应制得１。

A new synthetic method of a new tricyclic fluoroquinolone rufloxacin hydrochloride(1) is designed. This method has not been reported in literature in 32.5% yield. Rufloxacin hydrochloride has been prepared in eight steps from 2,3,4 trifluoronitrobenzene through substitution, reduction, bromization, cyclization, condensation cyclization, chelation, N methylpiperazination, and hydrolysis.