2-(2-氯乙氧基)乙酸叔丁酯 | 73834-55-6

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 2-(2-氯乙氧基)乙酸叔丁酯
• 英文名称: tert-butyl 2-(2-chloroethoxy)acetate
• CAS: 73834-55-6
• 化学式: C₈H₁₅ClO₃
• 分子量: 194.658
• InChiKey: WMVRQEMWJYRSNF-UHFFFAOYSA-N

物化性质

• 溶解度：
  可溶于氯仿、DMSO、己烷、甲醇

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  12
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.88
• 拓扑面积：
  35.5
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-(2-氯乙氧基)乙酸叔丁酯 在 盐酸 、 水 作用下， 反应 2.0h， 以95%的产率得到2-(2-氯乙氧基)乙酸
  参考文献：
  名称：

  WO2006/104646

  摘要：

  公开号：
• 作为产物：
  描述：

  溴乙酸叔丁酯 、 2-氯乙醇 在 sodium hydroxide 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以79%的产率得到2-(2-氯乙氧基)乙酸叔丁酯
  参考文献：
  名称：

  [EN] CARBOXYL SUBSTITUTED INDOLES FOR USE AS PPAR ALPHA MODULATORS
  [FR] INDOLES À SUBSTITUTION CARBOXYLE DESTINÉS À ÊTRE UTILISÉS EN TANT QUE MODULATEURS DU PPAR-ALPHA

  摘要：

  根据本发明提供了式(I)的新化合物或其药用可接受的盐或溶剂，其中R1和R2中的一个是H，另一个是COOH。这些化合物可用作PPAR调节剂。

  公开号：

  WO2009147121A1

文献信息

• [EN] POLYCYCLIC COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF RAPIDLY ACCELERATED FIBROSARCOMA POLYPEPTIDES<br/>[FR] COMPOSÉS POLYCYCLIQUES ET MÉTHODES POUR LA DÉGRADATION CIBLÉE DE POLYPEPTIDES DU FIBROSARCOME RAPIDEMENT ACCÉLÉRÉ
  申请人：ARVINAS OPERATIONS INC

  公开号：WO2020051564A1

  公开（公告）日：2020-03-12

  The present disclosure relates to bifunctional compounds, ULM— L—PTM, 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ULM—L—PTM，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）的调节剂具有实用性。具体而言，本公开涉及含有一端结合到相应E3泛素连接酶的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，另一端结合到目标蛋白RAF的部分，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：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。
• Process for preparing piperazine-substituted aliphatic carboxylates
  申请人：Salsbury Chemicals, Inc.

  公开号：US06239277B1

  公开（公告）日：2001-05-29

  A process is disclosed for the preparation of a piperazine-substituted aliphatic carboxylate having the formula where m and n are individually an integer of from 1 to 6, R and R′ are the same or different and are hydrogen, C1 to C6 alkyl or aryl or heteroaryl that is unsubstituted or is substituted with at least one substituent that is halo, C1 to C6 alkyl or C1 to C6 alkoxy and R″ is C3 to C12 branched alkyl or an organic or inorganic cation. The process comprises treating a solution comprising a compound of the formula wherein m, R and R′ are as defined above and an aliphatic ester of the formula X—(CH2)n—O—CH2—CO(O)R″ where X is a leaving group and n and R″ are as defined above, with an effective amount of a base for a time and at a temperature sufficient to form a piperazine-substituted aliphatic carboxylate. Hydrolysis of the carboxylate with acid produces a piperazine-substituted aliphatic carboxylic acid or the acid salt thereof.

  公开了一种制备含哌嗪取代的脂肪族羧酸酯的方法，其化学式为，其中m和n分别是1至6的整数，R和R′相同或不同，可以是氢、C1至C6的烷基或芳基或杂芳基，未取代或取代有至少一个卤素、C1至C6的烷基或C1至C6的烷氧基的取代基，且R″为C3至C12的支链烷基或有机或无机阳离子。该方法包括将化合物的溶液处理，所述化合物的化学式为，其中m，R和R′如上所定义，以及脂肪酸酯的化学式X—（CH2）n—O— —CO（O）R″，其中X是离去基，n和R″如上所定义，用足够量的碱在足够的时间和温度下处理，以形成含哌嗪取代的脂肪族羧酸酯。用酸水解羧酸酯可产生含哌嗪取代的脂肪族羧酸或其酸盐。
• Hiv Protease Inhibitors
  申请人：McLean Ed W.

  公开号：US20080194554A1

  公开（公告）日：2008-08-14

  The present invention features compounds that are HIV protease inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.

  本发明涉及一些化合物，它们是HIV蛋白酶抑制剂，因此在抑制HIV复制、预防和/或治疗HIV感染以及治疗艾滋病和/或ARC方面非常有用。
• 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。