甲磺酸帕珠沙星的合成  

Synthesis of pazufloxacin mesilate

作　　者：钱方[1] 黎文海[2] 

机构地区：[1]南京医科大学附属南京市第一医院药剂科,江苏南京210006 [2]中国药科大学,江苏南京210017

出　　处：《山西化工》2011年第3期7-9,34,共4页Shanxi Chemical Industry

摘　　要：研究了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-氧代-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、Hofmann降解、成盐,制得甲磺酸帕珠沙星,总收率49.4%。其化学结构经元素分析、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 studied. Compound was synthesized from （S） -9,10-ditluoro-3-methyl-2,3-dihydro-7-oxo-7-H-pyrido [ 1, 2,3-de ] [ 1,4 ] benzoxazine-6-carboxylate by nucleophilic substitution, hydrolysis and selective decarboxylation, cyclic addition, hydrolysis. Hofmann degradation and salt formation, its overall yield was 49.4%. The chemical structure was confirmed by elemental analysis, IR, ^1H NMR, ^13C NMR, MS. This synthetic routy was suitable for industrial production.

关 键 词：甲磺酸帕珠沙星 抗菌药 合成 

分 类 号：R978.1[医药卫生—药品] TQ463.54[医药卫生—药学]