4-aminomethylpyrrolidin-3-one O-methyloxime

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 4-aminomethylpyrrolidin-3-one O-methyloxime
• 英文别名: (Z)-4-(Aminomethyl)pyrrolidin-3-one O-methyl oxime；[(4Z)-4-methoxyiminopyrrolidin-3-yl]methanamine
• 化学式: C₆H₁₃N₃O
• 分子量: 143.189
• InChiKey: YZBFISOEIGOFAF-RMKNXTFCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  59.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-氨基-1-环丙基-6,7,8-三氟-4-氧代-1,4-二氢-3-喹啉羧酸 、 4-aminomethylpyrrolidin-3-one O-methyloxime 以40%的产率得到1-cyclopropyl-5-amino-6,8-difluoro-7-(4-aminomethyl-3-methyloxyiminopyrrolidin-1-yl)-4-oxo-1 4-dihydroquinoline-3-carboxylic acid
  参考文献：
  名称：

  7-(4-aminomethyl-3-methyloxyiminopyrroplidin-1-yl)-1-cyclopropyl-6-flu

  摘要：

  本发明涉及一种具有优异抗菌活性的新型喹诺酮化合物。更具体地说，本发明涉及由以下式表示的7-(4-氨甲基-3-甲氧基亚氨基吡咯啉-1-基)-1-环丙基-6-氟-4-氧-1,4-二氢-1,8-萘啶-3-羧酸：##STR1##或其异构体。

  公开号：

  US05776944A1

文献信息

• PROCESS FOR THE PREPARATION OF GEMIFLOXACIN
  申请人：Ramasubbu Chandrasekaran

  公开号：US20100076193A1

  公开（公告）日：2010-03-25

  The present invention relates to an improved process for the preparation of Gemifloxacin mesylate of formula (V). The present invention further provides novel intermediates of formula (II) and (IV), which are useful intermediates for the preparation of Gemifloxacin mesylate of formula (V). wherein R 1 is linear or branched chain alkyl group having 1-3 carbon atoms.

  本发明涉及一种改进的制备公式（V）的Gemifloxacin甲磺酸盐的过程。本发明还提供了公式（II）和（IV）的新型中间体，它们是制备公式（V）的Gemifloxacin甲磺酸盐的有用中间体。其中R1是具有1-3个碳原子的线性或支链烷基。
• Process for the preparation of amorphous gemifloxacin
  申请人：Hetero Drugs Limited

  公开号：EP2161269A1

  公开（公告）日：2010-03-10

  A process for the preparation of amorphous gemifloxacin comprising preparing a solution of gemifloxacin in dimethylformamide or methylene chloride, and isolating amorphous gemifloxacin from the solution.

  一种制备非晶态吉米沙星的方法，包括制备二甲基甲酰胺或氯甲烷中的吉米沙星溶液，并从溶液中分离非晶态吉米沙星。
• GEMIFLOXACIN PROCESS AND POLYMORPHS
  申请人：PARTHASARADHI REDDY Bandi

  公开号：US20110136855A1

  公开（公告）日：2011-06-09

  The present invention provides a novel process for the preparation of gemifloxacin and its pharmaceutically acceptable acid addition salts in high yield. The present invention also relates to novel polymorphs of gemifloxacin free base and its hydrates to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention also relates to infusion solutions of gemifloxacin and to processes for their preparation. Thus, 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphth-yridine-3-carboxylic acid is reacted with a mixture of acetic anhydride, acetic acid and boric acid to give borane compound, which is then treated with 4-Aminomethyl-3-methoxyimino-pyrrolidinium dimethanesulfonate in presence of triethylamine, followed by treatment with 3.5% sodium hydroxide solution to give gemifloxacin free base.

  本发明提供了一种制备吉米沙星及其药学上可接受的酸盐的新方法，其产率高。本发明还涉及吉米沙星游离碱的新多晶形态及其水合物的制备方法，以及包含它们的制药组合物。本发明还涉及吉米沙星的输注溶液及其制备方法。因此，7-氯-1-环丙基-6-氟-4-氧代-1,4-二氢-1,8-萘啉-3-羧酸与乙酸酐、乙酸和硼酸混合物反应，得到硼烷化合物，然后在三乙胺的存在下，用4-氨基甲基-3-甲氧基亚胺吡咯烷二甲磺酸盐处理，随后用3.5％的氢氧化钠溶液处理，得到吉米沙星游离碱。
• Gemifloxacin process and polymorphs
  申请人：Hetero Drugs Limited

  公开号：EP2159225A1

  公开（公告）日：2010-03-03

  Gemifloxacin lactate and gemiflxacin formate, processes for the preparation thereof and pharmaceutical compositions containing gemifloxacin lactate or gemiflxacin formate.

  Gemifloxacin乳酸盐和Gemiflxacin甲酸盐，其制备方法以及含有Gemifloxacin乳酸盐或Gemiflxacin甲酸盐的制药组合物。
• Gemifloxacin hydrates
  申请人：Hetero Drugs Limited

  公开号：EP2161270A1

  公开（公告）日：2010-03-10

  Gemifloxacin hemihydrate, monohydrate and sesquihydrate, processes for the preparation thereof and pharmaceutical compositions containing gemifloxacin hemihydrate, monohydrate and sesquihydrate.

  Gemifloxacin半水合物、单水合物和1.5倍水合物的制备方法及含有Gemifloxacin半水合物、单水合物和1.5倍水合物的药物组合物。