6-[4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]morpholin-3-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: 6-[4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]morpholin-3-one
• 化学式: C₁₄H₁₇N₃O₄
• 分子量: 291.3
• InChiKey: COZHAHIZHXFOKV-PXYINDEMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  93.9
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• NOVEL METHOD FOR SYNTHESIZING RIVAROXABAN INTERMEDIATE, 4-MORPHOLIN-3-ONE
  申请人：Zi Chunpeng

  公开号：US20140114066A1

  公开（公告）日：2014-04-24

  The present invention discloses novel methods for synthesizing Rivaroxaban intermediate, i.e., 4-4-[(5S)-5-(aminomethyl)-2-oxo-1,3 -oxazolidin-3 -yl]phenyl}morpholin-3-one. The novel methods provided in the present invention involve mild reaction conditions, convenient operations, easy purification, and low production costs, and thus the process is environmental-friendly and suitable for industrial production.

  本发明揭示了一种合成利伐沙班中间体的新方法，即4-4-[(5S)-5-(氨甲基)-2-氧代-1,3-噁唑烷-3-基]苯基}吗啉-3-酮。本发明提供的新方法涉及温和的反应条件、便捷的操作、易于纯化和低生产成本，因此该过程环保且适合工业生产。
• NOVEL METHOD FOR SYNTHESIZING RIVAROXABAN INTERMEDIATE, 4-{4-[(5S)-5-(AMINOMETHYL)-2-OXO-1,3-OXAZOLIGDIN-3-YL]PHENYL}MORPHOLIN-3-ONE
  申请人：Zhejiang Huahai Pharmaceutical Co., Ltd.

  公开号：EP2722330A1

  公开（公告）日：2014-04-23

  The present invention discloses novel methods for synthesizing Rivaroxaban intermediate, i.e., 4- 4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl} morpholin-3-one. The novel methods provided in the present invention involve mild reaction conditions, convenient operations, easy purification, and low production costs, and thus the process is environmental-friendly and suitable for industrial production.

  本发明公开了合成利伐沙班中间体，即4-4-[(5S)-5-(氨基甲基)-2-氧代-1,3-恶唑啉-3-基]苯基}吗啉-3-酮的新方法。本发明提供的新方法反应条件温和、操作简便、易于纯化、生产成本低，因此该工艺对环境友好，适合工业化生产。