芳基氟喹诺酮抗菌剂的合成新方法

提出了一种合成芳基氟喹诺酮抗菌剂二氟沙星和替马沙星的新方法，以2，4- 二氯-5氟苯乙酮为原料，用草酸二乙酯代替文献报道的碳酸二惭酯与之反应，高收 率得到β-酮酸酯，该酮酸酯经乙氧亚甲基化、胺化、环合和水解反应制得比文献 报道的类似物多一个羰基的中间本，再经过氧化物氧化脱羰基，与哌嗪衍生物缩合 制得标题化合物，所制得的新化合物的结构由~1H NMR, IR, MS和元素分析确证。

Novel Synthesis of Arylfluoroquinolone Antimicrobial Agents

A new synthetic method for preparing two arylfluoroquinolone antimicrobial agents, difloxacin and temafloxacin, was reported. 2,4- Dichloro-5-fluoroacetophenone was used as a starting material to react with diethyl oxalate in place of diethyl carbonate giving the corresponding β-keto ester in high yield. The β-keto ester was allowed to ethyloxymethenylation, amination, cyclization and hydrolysis to afford an intermediate acid with one more caxbonyl compared with that reported in the literature. After decarbonylation, it reacted with piperazine derivatives to yield the desired antibiotics. All new compounds were confirmed by 1H NMR, IR, MS spectra and elemental analysis.