S-(-)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic Acid D-arginine Salt | 627891-14-9

• 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: S-(-)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic Acid D-arginine Salt
• 英文别名: (2R)-2-amino-5-(diaminomethylideneamino)pentanoic acid;(12S)-7-fluoro-8-(4-hydroxypiperidin-1-yl)-12-methyl-4-oxo-1-azatricyclo[7.3.1.05,13]trideca-2,5,7,9(13)-tetraene-3-carboxylic acid
• CAS: 627891-14-9
• 化学式: C₆H₁₄N₄O₂*C₁₉H₂₁FN₂O₄
• 分子量: 534.588
• InChiKey: WIFOPRFVQIVWTB-KGZIKPOMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.76
• 重原子数：
  38
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  209
• 氢给体数：
  6
• 氢受体数：
  11

反应信息

• 作为产物：
  描述：

  D-精氨酸 、 左氧那地沙星 以 甲醇 、 水 为溶剂， 反应 0.25h， 以88%的产率得到S-(-)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic Acid D-arginine Salt
  参考文献：
  名称：

  CRYSTALLINE FLUOROQUINOLONE ARGININE SALT FORM

  摘要：

  本发明涉及RS-(±)-9-氟-6,7-二氢-8-(4-羟基哌啶-1-基)-5-甲基-1-氧代-1H,5H-苯并[i,j]喹啉-2-羧酸、S-(−)-9-氟-6,7-二氢-8-(4-羟基哌啶-1-基)-5-甲基-1-氧代-1H,5H-苯并[i,j]喹啉-2-羧酸、R-(+)-9-氟-6,7-二氢-8-(4-羟基哌啶-1-基)-5-甲基-1-氧代-1H,5H-苯并[i,j]喹啉-2-羧酸的新精氨酸盐形式，以及其制备方法和药物配方，其中该精氨酸盐形式作为活性成分用于治疗微生物感染。

  公开号：

  US20030225119A1

文献信息

• CRYSTALLINE FLUOROQUINOLONE ARGININE SALT FORM
  申请人：WOCKHARDT LIMITED

  公开号：US20030225119A1

  公开（公告）日：2003-12-04

  The invention relates to the new arginine salt forms of RS-(±)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, R-(+)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating microbial infections.

  本发明涉及RS-(±)-9-氟-6,7-二氢-8-(4-羟基哌啶-1-基)-5-甲基-1-氧代-1H,5H-苯并[i,j]喹啉-2-羧酸、S-(−)-9-氟-6,7-二氢-8-(4-羟基哌啶-1-基)-5-甲基-1-氧代-1H,5H-苯并[i,j]喹啉-2-羧酸、R-(+)-9-氟-6,7-二氢-8-(4-羟基哌啶-1-基)-5-甲基-1-氧代-1H,5H-苯并[i,j]喹啉-2-羧酸的新精氨酸盐形式，以及其制备方法和药物配方，其中该精氨酸盐形式作为活性成分用于治疗微生物感染。
• Crystalline fluoroquinolone arginine salt form
  申请人：Wockhardt Limited

  公开号：EP1918289A2

  公开（公告）日：2008-05-07

  The invention relates to the new arginine salt forms of RS-(±)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-l-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, S-(-)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, R-(+)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating microbial infections.

  本发明涉及 RS-(±)-9-氟-6,7-二氢-8-(4-羟基哌啶-1-基)-5-甲基-l-氧代-1H,5H-苯并[i、j]喹嗪-2-羧酸，S-(-)-9-氟-6,7-二氢-8-(4-羟基哌啶-1-基)-5-甲基-1-氧代-1H,5H-苯并[i,j]喹嗪-2-羧酸、R-(+)-9-氟-6,7-二氢-8-(4-羟基哌啶-1-基)-5-甲基-1-氧代-1H,5H-苯并[i,j]喹嗪-2-羧酸、它们的制备工艺以及包含这些精氨酸盐形式作为活性成分的药物制剂，用于治疗微生物感染。
• [EN] CRYSTALLINE FLUOROQUINOLONE ARGININE SALT FORM<br/>[FR] FORME CRISTALLINE DE SEL D'ARGININE DE FLUOROQUINOLONE
  申请人：WOCKHARDT LTD

  公开号：WO2003099815A1

  公开（公告）日：2003-12-04

  The invention relates to the new arginine salt forms of RS-(±)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, S-(-)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, R-(+)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating microbial infections.

  本发明涉及RS-(±)-9-氟-6,7-二氢-8-(4-羟基哌啶-1-基)-5-甲基-1-氧-1H,5H-苯并[i,j]喹啉-2-羧酸，S-(-)-9-氟-6,7-二氢-8-(4-羟基哌啶-1-基)-5-甲基-1-氧-1H,5H-苯并[i,j]喹啉-2-羧酸，R-(+)-9-氟-6,7-二氢-8-(4-羟基哌啶-1-基)-5-甲基-1-氧-1H,5H-苯并[i,j]喹啉-2-羧酸的新精氨酸盐形式，其制备方法和药物制剂，其中该精氨酸盐形式作为活性成分用于治疗微生物感染。