Gatifloxacin hemihydrate | 404858-36-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: Gatifloxacin hemihydrate
• 英文别名: 1-cyclopropyl-6-fluoro-8-methoxy-7-(3-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid;hydrate
• CAS: 404858-36-2
• 化学式: C38H46F2N6O9
• 分子量: 768.8
• InChiKey: ISCAXBHESPTGIQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.14
• 重原子数：
  55
• 可旋转键数：
  8
• 环数：
  8.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  165
• 氢给体数：
  5
• 氢受体数：
  17

文献信息

• [EN] AN IMPROVED PROCESS FOR THE PREPARATION OF GATIFLOXACIN<br/>[FR] PROCEDE AMELIORE DE PREPARATION DE GATIFLOXACINE
  申请人：MATRIX LAB LTD

  公开号：WO2005009970A1

  公开（公告）日：2005-02-03

  The present invention relates to a process for the preparation of Gatifloxacin by reacting ethvl 1-cyclopropyl-6,7-difluoro-8­ methoxy-4-oxo-1,4-dihydro-3-quinoline carboxylate with aqueous hydrofluoroboric acid followed by condensation with 2-methyl piperazine in polar organic solvent resulting in an intermediate Cyclopropyl-7-(3-methylpiperazin-1-yl)-6-fluoro-8-methoxy-4-oxo­ 1,4-dihydro-3-quinoline carboxylic acid boron difluoride chelate which upon hydrolysis yields Gatifloxacin.

  本发明涉及一种通过将乙酰1-环丙基-6,7-二氟-8-甲氧基-4-羰基-1,4-二氢-3-喹啉羧酸酯与水溶氢氟硼酸反应，然后在极性有机溶剂中与2-甲基哌嗪进行缩合反应得到中间体环丙基-7-(3-甲基哌嗪-1-基)-6-氟-8-甲氧基-4-羰基-1,4-二氢-3-喹啉羧酸硼二氟螯合物的制备方法，该中间体在水解后生成加替沙星。
• [EN] CRYSTALLINE FORM OF GATIFLOXACIN<br/>[FR] FORME CRISTALLINE DE GATIFLOXACINE
  申请人：SINT QUIMICA SA

  公开号：WO2005047262A1

  公开（公告）日：2005-05-26

  The present invention relates to a crystalline form of gatifoxacin (formula I) obtainable by process that comprises recrystallisation of the crude gatifloxacin in methanol and which is stable with a water content ranging between 2.5 and 4.5% by weight, to a process for preparing it and to the use thereof as an active substance in the preparation of pharmaceutical formulations.

  本发明涉及一种晶体形式的加替沙星（式I），该晶体形式可通过以下工艺获得：在甲醇中重结晶粗加替沙星，其稳定的水含量范围为2.5至4.5重量％，以及制备该晶体形式的工艺和将其用作制备制药配方中的活性物质的用途。
• Novel crystalline forms of gatifloxacin
  申请人：Parthasaradhi Bandi Reddy

  公开号：US20050085640A1

  公开（公告）日：2005-04-21

  The present invention relates to novel crystalline forms of gatifloxacin, to processes for their preparation and to pharmaceutical compositions containing them.

  本发明涉及新的吉他氧星晶体形式，其制备过程和含有它们的药物组成物。
• Novel crystalline forms of gatifloxacin and processes for preparation
  申请人：——

  公开号：US20040171621A1

  公开（公告）日：2004-09-02

  Provided are novel crystalline forms of gatifloxacin, some of which are DMSO solvates, and methods for making them.

  提供了新的吉他氧星晶体形式，其中一些是DMSO溶剂合物，并提供了制备方法。
• Novel crystalline forms of gatofloxacin and processes for preparation
  申请人：Amir Ehud

  公开号：US20060258675A1

  公开（公告）日：2006-11-16

  Provided are novel crystalline forms of gatifloxacin, some of which are DMSO solvates, and methods for making them.

  提供了新型晶体形态的加替沙星，其中一些是DMSO溶剂化物，并提供制备方法。