抗菌药甲磺酸帕珠沙星的合成

journal6 ›› 2009, Vol. 30 ›› Issue (5): 96-100.

抗菌药甲磺酸帕珠沙星的合成

（1.吉首大学党委宣传部，湖南吉首 416000；2.吉首大学化学化工学院，湖南吉首 416000）

出版日期:2009-09-25 发布日期:2012-04-21
通讯作者: 彭晓春（1964-），女（土家族），湖南永顺人，吉首大学化学化工学院教授，博士，主要从事高分子合成与改性研究.电话:0743-8564911.E-mail:pnfxz@126.com.
作者简介:申绪湘（1962-），女（土家族），吉林省敦化人，吉首大学副教授，主要从事药物化学研究
基金资助:
湖南省教育厅科学研究项目（07C519）

Synthesis of Antimicrobial Pazufloxacin Mesilate

(1.Party Committee Propaganda Department,Jishou University,Jishou 416000,Hunan China;2.Department of Chemistry and Chemical Engineering,Jishou University,Jishou 416000,Hunan China)

Online:2009-09-25 Published:2012-04-21

摘要/Abstract

摘要：以左旋氧氟沙星中间体（(S)-9,10-二氟-3-甲基-2,3-二氢-7-氧代-7-H-吡啶并[1,2,3-de][1,4]苯并噁嗪-6-羧酸乙酯）为起始原料，经亲核取代、选择性脱羧、环丙化、水解反应、Hofmann重排和成盐单元反应合成了甲磺酸帕珠沙星，经HPLC检测，质量浓度为91.352 g/L.优化后的工艺过程适合工业化批量生产.

关键词： 抗菌剂, 甲磺酸帕珠沙星, 合成

Abstract: 〗Pazufloxacin mesilate was synthesized from (S)-9,10-difluoro-3-methly-7-oxo-2,3-dihydro-7-H-pyrido[1,2,3-de][1,4] benzoxazine-6-carboxylate with nuclephilic substitution,selective decarboxylation,cyclic addition,hydrolysis,Hofmann recomposition and salt formation.The product was tested by HPLC and the results showed content of 91.352 g/L.The optimized process is suitable for industrial mass production.

Key words: antimicrobial, pazufloxacin mesilate, synthesis

申绪湘, 彭晓春, 龚兴浪, 肖竹平, 王迎春, 李志平. 抗菌药甲磺酸帕珠沙星的合成[J]. journal6, 2009, 30(5): 96-100.

SHEN Xu-Xiang, PENG Xiao-Chun, GONG Xing-Lang, XIAO Zhu-Ping, WANG Ying-Chun, LI Zhi-Ping. Synthesis of Antimicrobial Pazufloxacin Mesilate[J]. journal6, 2009, 30(5): 96-100.

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