(5R)-7-Methyl-2-[4-methyl-6-[4-(trifluoromethyl)phenyl]pyrimidin-2-yl]-1,7-diazaspiro[4.4]non-1-en-6-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: (5R)-7-Methyl-2-[4-methyl-6-[4-(trifluoromethyl)phenyl]pyrimidin-2-yl]-1,7-diazaspiro[4.4]non-1-en-6-one
• 英文别名: (5R)-7-methyl-2-[4-methyl-6-[4-(trifluoromethyl)phenyl]pyrimidin-2-yl]-1,7-diazaspiro[4.4]non-1-en-6-one
• 化学式: C₂₀H₁₉F₃N₄O
• 分子量: 388.4
• InChiKey: CIBIQCRUDYBRJO-LJQANCHMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  28
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  58.4
• 氢给体数：
  0
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  (3R)-3-amino-1-methyl-3-[3-[4-methyl-6-[4-(trifluoromethyl)phenyl]pyrimidin-2-yl]prop-2-ynyl]pyrrolidin-2-one 在 silver trifluoromethanesulfonate 氨 、 甲醇 、 乙酸乙酯 作用下， 以 乙腈 为溶剂， 反应 108.0h， 以affording (5R)-7-methyl-2-[4-methyl-6-[4-(trifluoromethyl)phenyl]pyrimidin-2-yl]-1,7-diazaspiro[4.4]non-1-en-6-one (D15) (359 mg, 0.924 mmol) as a light brown solid with a few % of impurities present的产率得到(5R)-7-Methyl-2-[4-methyl-6-[4-(trifluoromethyl)phenyl]pyrimidin-2-yl]-1,7-diazaspiro[4.4]non-1-en-6-one
  参考文献：
  名称：

  Pyrimidinyl-diazospiro compounds

  摘要：

  本发明涉及螺环衍生物，以及利用该衍生物治疗通过调节电压门控钠通道介导的疾病和病症，包含该衍生物的组合物和其制备过程。

  公开号：

  US09309254B2

文献信息

• NOVEL COMPOUNDS
  申请人：CONVERGANCE PHARMACEUTICALS LIMITED

  公开号：US20150119404A1

  公开（公告）日：2015-04-30

  The invention relates to spiro derivatives, to the use of said derivatives in treating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation.

  本发明涉及螺环衍生物，其在治疗通过调节电压门控钠通道介导的疾病和病状中的应用，以及含有该衍生物的组合物和其制备过程。
• Novel Pyrimidinyl-DiazoSpiro Compounds
  申请人：CONVERGENCE PHARMACEUTICALS LIMITED

  公开号：US20160184306A1

  公开（公告）日：2016-06-30

  The invention relates to spiro derivatives, to the use of said derivatives in treating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation.

  本发明涉及螺内酯衍生物，涉及使用该衍生物治疗通过调节电压门控钠通道介导的疾病和病症，涉及含有该衍生物的组合物以及其制备方法。
• US9309254B2
  申请人：——

  公开号：US9309254B2

  公开（公告）日：2016-04-12
• [EN] NOVEL COMPOUNDS<br/>[FR] NOUVEAUX COMPOSÉS
  申请人：CONVERGENCE PHARMACEUTICALS

  公开号：WO2013175206A1

  公开（公告）日：2013-11-28

  The invention relates to spiro derivatives, to the use of said derivatives in treating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation.
• Pyrimidinyl-diazospiro compounds
  申请人：CONVERGENCE PHARMACEUTICALS LIMITED

  公开号：US09309254B2

  公开（公告）日：2016-04-12

  The invention relates to spiro derivatives, to the use of said derivatives in treating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation.

  本发明涉及螺环衍生物，以及利用该衍生物治疗通过调节电压门控钠通道介导的疾病和病症，包含该衍生物的组合物和其制备过程。