3-(4-methoxy-phenyl)-propionic acid ethylamide | 100369-80-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 3-(4-methoxy-phenyl)-propionic acid ethylamide
• 英文别名: 3-(4-Methoxy-phenyl)-propionsaeure-aethylamid；N-ethyl-3-(4-methoxyphenyl)propanamide
• CAS: 100369-80-0
• 化学式: C₁₂H₁₇NO₂
• mdl: MFCD03384184
• 分子量: 207.272
• InChiKey: KNZVOLHPDHKXLT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  15
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.416
• 拓扑面积：
  38.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  3-(4-methoxy-phenyl)-propionic acid ethylamide 在 N-碘代丁二酰亚胺 作用下， 以 二氯甲烷 为溶剂， 以23 %的产率得到1-ethyl-1-azaspiro[4.5]deca-6,9-diene-2,8-dione
  参考文献：
  名称：

  可见光诱导苯酚衍生物的无催化剂脱芳香酰胺化

  摘要：

  在此，概述了可见光诱导苯酚衍生物脱芳酰胺化反应的简单方案，以提供具有广泛底物范围的螺内酰胺。研究发现，酰胺化反应在室温下无需任何光催化剂即可顺利进行，并以 23%–87% 的产率获得了所需的螺内酰胺。显示出良好的官能团耐受性和广泛的底物范围

  DOI：

  10.1016/j.tetlet.2023.154637
• 作为产物：
  描述：

  N-Ethyl-5-chlormethylen-rhodamin 在 四氢呋喃 、 二硫化碳 、 三氯化铝 、 镍 作用下， 生成 3-(4-methoxy-phenyl)-propionic acid ethylamide
  参考文献：
  名称：

  Behringer et al., Chemische Berichte, 1958, vol. 91, p. 2773,2783

  摘要：

  DOI：

文献信息

• COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF RAPIDLY ACCELERATED FIBROSARCOMA POLYPEPTIDES
  申请人：Arvinas, Inc.

  公开号：US20180179183A1

  公开（公告）日：2018-06-28

  The present disclosure relates to bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.

  本公开涉及双功能化合物，其作为快速加速纤维肉瘤（RAF，如c-RAF、A-RAF和/或B-RAF；目标蛋白）的调节剂而发挥作用。具体而言，本公开涉及含有一端为Von Hippel-Lindau、cereblon、凋亡抑制蛋白或鼠双分子同源物2配体的双功能化合物，该配体与相应的E3泛素连接酶结合，并且另一端含有结合目标蛋白RAF的基团，使得目标蛋白与泛素连接酶靠近，以实现目标蛋白的降解（和抑制）。本公开展示了与目标蛋白的降解/抑制相关的广泛药理活性范围。本公开的化合物和组合物用于治疗或预防由目标蛋白的聚集或积累，或目标蛋白的构成性激活导致的疾病或紊乱。
• Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
  申请人：Arvinas, Inc.

  公开号：US10723717B2

  公开（公告）日：2020-07-28

  The present disclosure relates to bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.

  本公开涉及双功能化合物，它们可用作快速加速纤维肉瘤（RAF，如c-RAF、A-RAF和/或B-RAF；靶蛋白）的调节剂。特别是，本公开内容涉及双功能化合物，其一端含有与相应 E3 泛素连接酶结合的 Von Hippel-Lindau、cereblon、抑制细胞凋亡蛋白或小鼠双敏同源物 2 配体，另一端含有与靶蛋白 RAF 结合的分子，从而将靶蛋白置于泛素连接酶附近，以实现对靶蛋白的降解（和抑制）。本公开物具有与降解/抑制靶蛋白相关的广泛药理活性。本公开的化合物和组合物可以治疗或预防由于靶蛋白的聚集或积聚或靶蛋白的组成性激活而导致的疾病或失调。
• [EN] NOVEL 1,2,3,4,4a,5,6,7,8,9,10,10a-DODECAHYDROBENZO[G]QUINOLIN-6-OL COMPOUNDS AND USES THEREOF<br/>[FR] NOUVEAUX COMPOSÉS DE 1,2,3,4,4A,5,6,7,8,9,10,10A-DODÉCAHYDROBENZO[G]QUINOLIN-6-OL ET LEURS UTILISATIONS
  申请人：[en]INTEGRATIVE RESEARCH LABORATORIES SWEDEN AB

  公开号：WO2023208865A1

  公开（公告）日：2023-11-02

  There is disclosed a compound of Formula (II), a method of manufacturing thereof as well as uses thereof.
• [EN] NOVEL 1,2,3,4,4a,5,8,9,10,10a-DECAHYDROBENZO[G]QUINOLIN-6(7H)-ONE COMPOUNDS AND USES THEREOF<br/>[FR] NOUVEAUX COMPOSÉS DE 1,2,3,4,4A,5,8,9,10,10A-DÉCAHYDROBENZO[G]QUINOLIN-6(7H)-ONE ET LEURS UTILISATIONS
  申请人：[en]INTEGRATIVE RESEARCH LABORATORIES SWEDEN AB

  公开号：WO2023208867A1

  公开（公告）日：2023-11-02

  There is disclosed a compound of Formula (I), a method of manufacturing thereof as well as uses thereof.
• Behringer et al., Chemische Berichte, 1958, vol. 91, p. 2773,2783
  作者：Behringer et al.

  DOI：——

  日期：——