盐酸替马沙星的新法合成

Novel Process for Preparation of Temafloxacin Hydrochloride

以 2 ,4-二氯 - 5-氟苯甲酰乙酸乙酯为原料 ,经缩合 ,胺化 ,环合 ,螯合 ,取代 ,水解及成盐反应合成盐酸替马沙星。经元素分析 ,红外光谱 ,质谱和核磁共振谱确证结构 ,总收率 45%。该工艺路线副反应少 ,产品纯度高。

In search for more reasonable process for preparation of polyfluorated quinolone antibacterial agents, temafloxacin hydrochloride is prepared from ethyl 2,4 dichloro 5 fluorobenzoylacetate, via condensation, amination, cyclization, boron esterification, substitution, hydrolysis and salt formation with 45% overall yield. The structure of temafloxacin hydrochloride is confirmed by MS, 1H NMR, IR and EA.