第 45 卷第 5 期 Vol. 45 No. 5 2015 年 10 月 Oct 2015

所属栏目：医药及中间体 西他沙星及其有关物质D-2的合成

陈言德，杨 勇，周士阔，吕晓霞 （江苏吴中医药集团有限公司，江苏 苏州 215168）

摘　要：合成了西他沙星及其有关物质D-2，总收率78.7%。并对其进行了MS、HNMR和TG等表征；研究了氢化脱苄的反应条件、缩合反应的后处理优化和脱Boc的盐酸用量，优化的条件为：脱苄反应10%钯炭，回流反应0.5 h，缩合反应后处理溶剂比例v（乙腈）∶v（水）=1∶2，脱Boc的盐酸用量为15 mol倍量。

关键词：西他沙星；D-2；氢化；脱苄

中图分类号：R978.5　　文献标识码：A　　文章编号：1009-9212（2015）05-0030-04

Synthesis of Sitafloxacin and Its Related Substance D-2

CHEN Yan-de, YANG Yong, ZHOU Shi-kuo, L?譈 Xiao-xia (Jiangsu wuzhong pharmaceutical group, Suzhou 215168, China)

Abstract：Sitafloxacin and its related substance D-2 were obtained with a total product yield of 78.7%. The structures of Sitafloxacin and intermediates from the step reactions were confirmed using MS, HNMR and TG. The optimal conditions for each step reaction were as following: in the debenzylation reaction,10% of Pd/C with a reflux time of 0.5 h was adopted; in the post-treatment of condensation reaction, a mixed solvent of water and acetonitrile with a volume ratio of 2∶1 was used; in the deprotection of N-boc reaction, the amount of hydrochloric acid was 15 times of the substrate in mole.

Key words：sitafloxacin; D-2; hydrogenation; debenzylation

基金项目：苏州市科技发展计划项目（ZXY2012004）。

作者简介：陈言德（1984-），男，江苏泗洪人，工程师，硕士，主要从事化学药物开发工作（E-mail：chenyande86@163.com）。

收稿日期： 2015-08-2