2-甲氧基-4-(吡啶-2-基甲氧基)苯甲醛 | 1151539-21-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 2-甲氧基-4-(吡啶-2-基甲氧基)苯甲醛
• 英文名称: 2-methoxy-4-(2-pyridylmethoxy)benzaldehyde
• 英文别名: 2-Methoxy-4-(pyridin-2-ylmethoxy)benzaldehyde；2-methoxy-4-(pyridin-2-ylmethoxy)benzaldehyde
• CAS: 1151539-21-7
• 化学式: C₁₄H₁₃NO₃
• 分子量: 243.262
• InChiKey: JJBZSLAQDWDRGJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  18
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  48.4
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (E)-6-(1H-indol-6-yl)hex-5-ene-2,4-dione 、 2-甲氧基-4-(吡啶-2-基甲氧基)苯甲醛 在 boron trioxide 、 硼酸三异丙酯 、 哌啶 、 盐酸 作用下， 以 乙酸乙酯 、 水 为溶剂， 反应 2.0h， 以32%的产率得到(1E, 6E)-1-(1H-indol-6-yl)-7-[2-methoxy-4-(2-pyridylmethoxy)phenyl]hepta-1,6-diene-3,5-dione
  参考文献：
  名称：

  Design and synthesis of curcumin derivatives as tau and amyloid β dual aggregation inhibitors

  摘要：

  Alzheimer's disease (AD) is the most common form of dementia. In an AD patient's brain, senile plaques and neurofibrillary tangles, the abnormal aggregates of amyloid beta (A beta) peptide and tau protein, are observed as the two major hallmarks of this disease. To develop a new drug for treatment of AD, we have designed and synthesized a series of curcumin derivatives and evaluated their inhibitory activities against both tau and Ab aggregation. In this study, we describe the development of the more potent aggregation inhibitor 3-[(1E)-2-(1H-indol-6-yl) ethenyl]-5-[(1E)-2-[ 2-methoxy-4-(2-pyridylmethoxy) phenyl] ethenyl]-1H-pyrazole (compound 4, PE859). This compound has a better pharmacokinetic profile and pharmacological efficacy in vivo than curcumin, making it suitable as a drug for AD. (C) 2016 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2016.08.092
• 作为产物：
  描述：

  4-羟基-2-甲氧基苯甲醛 、 2-氯甲基吡啶盐酸盐 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 4.0h， 以82%的产率得到2-甲氧基-4-(吡啶-2-基甲氧基)苯甲醛
  参考文献：
  名称：

  NOVEL PYRAZOLE DERIVATIVE

  摘要：

  公开号：

  EP2698368B1

文献信息

• Pyrazole derivative
  申请人：Sugimoto Hachiro

  公开号：US09399635B2

  公开（公告）日：2016-07-26

  Provided is a novel therapeutic means for Alzheimer's disease. In particular, provided is a compound represented by the following general formula (I): [wherein Ar1 represents 2-methoxy-4-(2-pyridylmethoxy)phenyl etc. and Ar2 represents a 1H-indol-6-yl group etc.] or a salt thereof.

  提供了一种治疗阿尔茨海默病的新型治疗方法。特别地，提供了一种由以下一般式(I)所代表的化合物：[其中Ar1代表2-甲氧基-4-(2-吡啶基甲氧基)苯基等，Ar2代表1H-吲哚-6-基团等]或其盐。
• US9399635B2
  申请人：——

  公开号：US9399635B2

  公开（公告）日：2016-07-26
• Design and synthesis of curcumin derivatives as tau and amyloid β dual aggregation inhibitors
  作者：Michiaki Okuda、Ichiro Hijikuro、Yuki Fujita、Takayuki Teruya、Hirochika Kawakami、Takashi Takahashi、Hachiro Sugimoto

  DOI：10.1016/j.bmcl.2016.08.092

  日期：2016.10

  Alzheimer's disease (AD) is the most common form of dementia. In an AD patient's brain, senile plaques and neurofibrillary tangles, the abnormal aggregates of amyloid beta (A beta) peptide and tau protein, are observed as the two major hallmarks of this disease. To develop a new drug for treatment of AD, we have designed and synthesized a series of curcumin derivatives and evaluated their inhibitory activities against both tau and Ab aggregation. In this study, we describe the development of the more potent aggregation inhibitor 3-[(1E)-2-(1H-indol-6-yl) ethenyl]-5-[(1E)-2-[ 2-methoxy-4-(2-pyridylmethoxy) phenyl] ethenyl]-1H-pyrazole (compound 4, PE859). This compound has a better pharmacokinetic profile and pharmacological efficacy in vivo than curcumin, making it suitable as a drug for AD. (C) 2016 Elsevier Ltd. All rights reserved.
• NOVEL PYRAZOLE DERIVATIVE
  申请人：Green Tech Co., Ltd.

  公开号：EP2698368B1

  公开（公告）日：2018-02-14