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.
Pazufloxacin mesilate was synthesized from（S）-9,10-difluoro-3-methly-7-oxo-2,3-dihydro-7-H-pyrido[1,2,3-de] 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.
出处
《吉首大学学报（自然科学版）》
CAS
2009年第5期96-100,共5页
Journal of Jishou University(Natural Sciences Edition)
基金
湖南省教育厅科学研究项目(07C519)
关键词
抗菌剂
甲磺酸帕珠沙星
合成
antimicrobial
pazufloxacin mesilate
synthesis
