(2S)-2-(4-fluorophenyl)morpholine | 790655-16-2

• 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: (2S)-2-(4-fluorophenyl)morpholine
• CAS: 790655-16-2
• 化学式: C₁₀H₁₂FNO
• 分子量: 181.21
• InChiKey: MPFUBIGEMDOEIW-SNVBAGLBSA-N

物化性质

• 沸点：
  276.6±35.0 °C(Predicted)
• 密度：
  1.119±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  21.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-氯-1-甲基-[4,4-Bi嘧啶]-6(1H)-酮 、 (2S)-2-(4-fluorophenyl)morpholine 在 三乙胺 作用下， 以 四氢呋喃 为溶剂， 以74%的产率得到UDA-680
  参考文献：
  名称：

  WO2007/11065

  摘要：

  公开号：
• 作为产物：
  描述：

  (2S)-4-苄基-2-(4-氟苯基)吗啉 在 5%-palladium/activated carbon 氢气 作用下， 以 乙醇 为溶剂， 反应 1.0h， 以94%的产率得到(2S)-2-(4-fluorophenyl)morpholine
  参考文献：
  名称：

  WO2007/11065

  摘要：

  公开号：

文献信息

• 2-SUBSTITUTED-6-HETEROCYCLIC PYRIMIDONE DERIVATIVES AS TAU PROTEIN KINASE 1 INHIBITORS
  申请人：Watanabe Kazutoshi

  公开号：US20100113775A1

  公开（公告）日：2010-05-06

  A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein each R 1 represents hydrogen atom or the like; X represents oxygen atom or the like; A represents a C 3 -C 7 cycloalkyl group, a C 6 -C 10 aryl group or a heterocyclic group; R 6 represents a halogen atom or the like; s represents 0 or an integer of 1 to 5; Q represents a pyridine ring which may be substituted or pyrimidine ring; and R 2 represents hydrogen atom or the like, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).

  化合物的化学式为(I)，其光学活性异构体或药物可接受的盐：其中每个R1代表氢原子或类似物；X代表氧原子或类似物；A代表C3-C7环烷基，C6-C10芳基或杂环基；R6代表卤素原子或类似物；s代表0或1到5的整数；Q代表可能被取代的吡啶环或嘧啶环；R2代表氢原子或类似物，用于预防和/或治疗由tau蛋白激酶1的异常活性引起的疾病，如神经退行性疾病（例如阿尔茨海默病）。
• Intermediate compound for synthesizing pharmaceutical agent and production method thereof
  申请人：Mitsubishi Tanabe Pharma Corporation

  公开号：US07994315B2

  公开（公告）日：2011-08-09

  Production method of an optically active morpholine compound represented by the formula 10, or a compound represented by the formula 55, which includes the following steps: or wherein each symbol is as defined in the specification. An optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4′]bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.

  一种光学活性的吗啡啶化合物的生产方法，其化学式为10，或化学式为55的化合物，包括以下步骤：或其中每个符号如规范中所定义。通过一种工业上有利的方法，可以高产地生产重要的起始材料2-芳基取代吗啡啶化合物和3-氧代-3-(嘧啶-4-基)丙酸酯，用于合成具有tau蛋白激酶1抑制活性的2-(2-芳基吗啡啶-4-基)-1-甲基-1H-[4,4′]联吡啶-6-酮，该化合物可用作治疗阿尔茨海默病等疾病的治疗药物。
• INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF
  申请人：OKUYAMA Masahiro

  公开号：US20110251385A1

  公开（公告）日：2011-10-13

  The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: wherein each symbol is as defined in the specification. The present invention also relates to a production method of an compound represented by the formula 55, which includes the following steps: wherein each symbol is as defined in the specification. According to the production method of the present invention, an optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4′]bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.

  本发明涉及一种光学活性吗啉化合物的生产方法，其由公式10表示，包括以下步骤：其中每个符号如规范中所定义。本发明还涉及一种由公式55表示的化合物的生产方法，其包括以下步骤：其中每个符号如规范中所定义。根据本发明的生产方法，可以通过一种工业上有利的方法高产地生产重要的起始材料，即光学活性2-芳基取代吗啉化合物和3-氧代-3-(嘧啶-4-基)丙酸酯，用于合成具有tau蛋白激酶1抑制活性的2-(2-芳基吗啉-4-基)-1-甲基-1H-[4,4′]联吡啶基-6-酮，该化合物对阿尔茨海默病等有用作用的治疗药物。
• PYRIMIDONE COMPOUNDS
  申请人：Sakai Daiki

  公开号：US20120220591A1

  公开（公告）日：2012-08-30

  A pyrimidone derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof: wherein X represents hydrogen atom and Y represents hydroxyl group, or X represents fluorine atom and Y represents hydrogen atom; R 1 represents a C 1-6 alkyl group; R 2 represents a morpholin-4-yl group which may be substituted, or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).

  一种以一般式(I)表示的吡啶酮衍生物或其药学上可接受的盐：其中X代表氢原子，Y代表羟基；或X代表氟原子，Y代表氢原子；R1代表C1-6烷基；R2代表可被取代的吗啡啶-4-基团等，用于预防和/或治疗由tau蛋白激酶1过度活化引起的疾病，如神经退行性疾病（例如阿尔茨海默病）。
• NOVEL MORPHOLINYL DERIVATIVES USEFUL AS MOGAT-2 INHIBITORS
  申请人：Eli Lilly and Company

  公开号：US20150005305A1

  公开（公告）日：2015-01-01

  The present invention provides compounds of Formula I or a pharmaceutical salt thereof, methods of treating hypertriglyceridemia using the compounds; and a process for preparing the compounds.

  本发明提供了I式化合物或其药用盐，使用这些化合物治疗高甘油三酯血症的方法；以及制备这些化合物的过程。