摘要
研究氟喹诺酮类抗菌剂甲磺酸帕珠沙星的合成路线及工艺。以左旋氧氟沙星的中间体(S)-9,10-二氟-3-甲基-2,3-二氢-7-氧-7H-吡啶[1,2,3-de][1,4]苯并噁嗪-6-羧酸乙酯为起始原料,经亲核取代反应、酯水解并选择性脱羧、环合、水解、Hofrnann降解、成盐得甲磺酸帕珠沙星,总收率60.0%。其化学结构经元素分析,IR,1H NMR,13C NMR,MS得以确证。该合成路线及工艺适合工业化大生产。
The synthetic route and improved process for the preparation of pazufloxacin mesilate were stud-ied.Compound was synthesized from （S）-9,10-difluoro-3-methyl-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de] [1,4]benzoxazine-6-carboxylate by nucleophilic substitution, hydrolysis and selective decarboxyla-tion,cyclic addition, hydrolysis.Hofmann degradation and salt formation,its overall yield was60.0%.The chemical structure was confirmed by elemental analysis,IR,^1H NMR,^13C NMR,MS.This synthetic route is suitable for industrial manufacture.
出处
《应用化工》
CAS
CSCD
2007年第5期472-474,共3页
Applied Chemical Industry
关键词
氟喹诺酮类抗菌剂
甲磺酸帕珠沙星
合成
fluoroquinoione antibacterial agent
pazufloxacin mesilate
synthesis
