N-甲基盐酸莫西沙星的合成及在生产中的应用

Synthesis of N-Methyl Moxifloxacin Hydrochloride and Its Application in Production

以喹啉羧酸乙酯为原料,经硼酯化保护,与侧链缩合,脱保护成盐,然后与甲醛反应得目标产物N甲基盐酸莫西沙星(1-环丙基-7-(S,S-N-甲基-2,8-二氮杂双环[4.3.0]壬烷-8-基)-6-氟-8-甲氧基1,4-二氢-4-氧代-3-喹啉羧酸盐酸盐),化合物的结构通过ESI-MS、^(1)H NMR、^(13)C NMR进行确认,并研究其在生产监控和质量标准中的应用。

N-methyl moxifloxacin hydrochloride （1-cyclopropyl-6-fluoro-1, 4-dihydro-8-methoxy-7-[（4aS,7aS）-N-methy-octahydro-6H-pyrrolo [3,4-b] pyridin-6-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylic acidhydrochloride） was synthesized with quinoline carboxylic ethyl ester as starting materials via esterifica-tion protection, condensation with side chain and reaction with formaldehyde after deprotecting. Thetarget compound was characterized by ESI-MS, 1H NMR and 13C NMR. The applying in production mo-nitoring and quality standardof the compound was also studied.