CAJ | 학술논문

目的：合成西他沙星。方法以2，4，5-三氟苯甲酰乙酸乙酯为起始原料，经缩合、取代、环合、水解、7位取代、8位氯代、脱保护基等7步反应制得目标化合物。结果目标化合物结构经1H NMR、MS确证，并与文献报道一致，总收率为69.8％，纯度为99.9％（HPLC法）。结论本工艺操作简单，产品质量好，适合工业化生产。
목적：합성서타사성。방법이2，4，5-삼불분갑선을산을지위기시원료，경축합、취대、배합、수해、7위취대、8위록대、탈보호기등7보반응제득목표화합물。결과목표화합물결구경1H NMR、MS학증，병여문헌보도일치，총수솔위69.8％，순도위99.9％（HPLC법）。결론본공예조작간단，산품질량호，괄합공업화생산。
OBJECTIVE To synthesize sitafloxacin.METHODS The target compound was synthesized via seven steps including condensation ,substitution ,cyclization ,hydrolysis ,7-substitution ,8-chlorination and deprotection employing ethyl 2,4,5-trifluorobenzoyl acetate as a starting material.RESULTS The structure of the target com-pound was confirmed by 1H NMR and MS, and consistent with the literature.The total yield of sitafloxacin was 69.8%,HPLC purity was 99.9%.CONCLUSION A high-quality and simple method which can be used in the in-dustrial production is achieved.