甲磺酸帕珠沙星的合成

Synthesis of Pazufloxacin Mesilate

[目的 ]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。 [方法 ]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]苯并口恶嗪 - 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 ,成盐得甲磺酸帕珠沙星 ,总收率 42 .7%。[结果 ]合成了目标化合物 ,其化学结构经元素分析 ,IR,1 HNMR,1 3 CNMR,MS得以确正。 [结论

To study an improved process for the preparation of pazufloxacin mesilate(1) . Compound (1) was synthesized from (s)-9,10-difluoro-3-methyl-7-oxo-2,3-dihydro-7H-pyridobenzoxazine-6-carboxylate(2) by nucleophilic substitution, hydrolysis and selective decarboxylation, cyclic addition, hydrolysis, Hofmann degradation and salt formation. The overall yield was 42.7%. The constitution of 1 was confirmed by elemental analysis, IR, +1HNMR, +{13}CNMR, MS.[CONCLUSION] This synthesis is suitable for industrial manufacture.