第 47 卷第 1 期 Vol. 47 No. 1 2017 年 2 月 Feb 2017

所属栏目：医药及中间体 一种德拉沙星的制备方法

王秀娟，郭彦玲 （鲁南制药集团，山东 临沂 276002）

摘　要：以2，4，5-三氟苯甲酰乙酸乙酯为起始物，经缩合、氯代、水解制得德拉沙星，其中氯代反应考察了提纯方法，使5位氯代物杂质减少；水解反应优化水解条件，使氧化杂质减少。用该方法制得的德拉沙星纯度大于99.8%，5位氯代杂质和氧化杂质均小于0.1%，满足药用要求。操作简单，对设备无苛刻要求，具有工业化应用前景。

关键词：德拉沙星；2，4，5-三氟苯甲酰乙酸乙酯；5位氯代杂质；氧化杂质

中图分类号：0625.2　　文献标识码：A　　文章编号：1009-9212（2017）01-0056-04

Preparation of Delafloxacin

WANG Xiu-juan, GUO Yan-ling (Lunan Pharmaceutical Group Corporation, Linyi 276002, China)

Abstract：This article reported a method for the preparation of Delafloxacin, which had advantages including simple operation-process, no rigid requirements for equipment, high yield and high purity of final product. All advantages made this method suitable for industrial production. In this method, ethyl 2,4,5-trifluorobenzoylacetate was selected as the starting material, and the final product was obtained through reactions including condensation, chlorination, hydrolysis. In the manufacturing process, the purification method for chlorination had been studied to reduce 5-chlorinated impurity, meanwhile, the conditions for hydrolysis had been optimized to reduce the amount of oxidant. Through all of the improvements, Delafloxacin obtained in this method had very high quality with a purity more than 99.8%, both 5-chlorinated and oxidant impurity were less than 0.1%.

Key words：Delafloxacin; ethyl 2,4,5-trifluorobenzoylacetate; 5-chlorinated impurity; oxidant impurity

作者简介：王秀娟（1980-），女，山东潍坊人，工程师，研究方向：药物研发（E-mail:xiujuan0103@163.com）。

收稿日期：2017-02-13