2-(2-chloroethoxy)ethyl tosylate | 64820-21-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-(2-chloroethoxy)ethyl tosylate
• 英文别名: 2-(2-chloroethoxy)ethyl 4-methylbenzenesulfonate；2-(2-chloroethoxy)ethyl p-toluenesulfonate；Chloroethoxyethyl-tosylate
• CAS: 64820-21-9
• 化学式: C₁₁H₁₅ClO₄S
• 分子量: 278.757
• InChiKey: SWPSLRINHOQENG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  17
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  61
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-(2-chloroethoxy)ethyl tosylate 、 (E)-4-Phenylazophenol 在 potassium carbonate 作用下， 以 乙腈 为溶剂， 反应 24.0h， 以82%的产率得到(E)-1-{4-[2-(2-chloroethoxy)ethoxy]phenyl}-2-phenyldiazene
  参考文献：
  名称：

  囊泡的光响应分子识别和粘附

  摘要：

  超分子胶：双官能偶氮苯的光诱导异构化可用于诱导和逆转由环糊精（CD）分子组成的双层囊泡的分子识别和粘附。这种光响应性超分子胶的分子基础是偶氮苯的顺式-反式异构化（见图）；黑圈CD，绿色反式-偶氮苯，红色顺式-偶氮苯）。

  DOI：

  10.1002/anie.201001442
• 作为产物：
  描述：

  2-氯乙氧基乙醇 、 对甲苯磺酰氯 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 生成 2-(2-chloroethoxy)ethyl tosylate
  参考文献：
  名称：

  18F-氟化新戊二醇侧链对二苯乙烯淀粉样蛋白-β PET配体生物学特性的影响

  摘要：

   介绍 2,2-二羟甲基-1-[ 18 F]氟丙烷基团，也称为18 F-标记的新戊二醇侧链，是一种用于正电子发射断层扫描 (PET) 成像剂的新型18 F-标记基团。该小组的目的是开发无需高效液相色谱的固相萃取简单纯化方法。然而，新戊基18 F 标记基团对脑成像剂特性的影响尚不清楚。在这里，我们将该侧链添加到具有氨基芪结构的化合物中，以评估其对氨基芪作为淀粉样蛋白-β (Aβ)放射性配体的生物学特性的影响。  方法 四种新型18 F 标记二苯乙烯化合物（具有不同长度的聚乙二醇 (PEG) 连接体，称为 [ 18 F]Cpd-0、-1、-2 和 -4，（PEG = 0、1、2 和4) 和[ 18 F]AV-1 在正常小鼠中进行了评估。使用小鼠血浆和脑进行[ 18 F]Cpd-0和-1的代谢分析。进行[ 18 F]AV-1 与 Aβ 1 – 42原纤维结合的竞争性结合测定，以确定化合物的结合特性。

  DOI：

  10.1016/j.nucmedbio.2020.12.008

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。
• THIAZOLIDINONE COMPOUNDS AND USE THEREOF
  申请人：National Health Research Institutes

  公开号：US20170253569A1

  公开（公告）日：2017-09-07

  A pharmaceutical composition containing a compound of Formula (I) for treating an opioid receptor-associated condition. Also disclosed is a method for treating an opioid receptor-associated condition using such a compound. Further disclosed are two sets of thiazolidinone compounds of formula (I): (i) compounds each having an enantiomeric excess greater than 90% and (ii) compounds each being substituted with deuterium.

  一种含有化合物（I）的药物组合物，用于治疗与阿片受体相关的疾病。还公开了一种使用这种化合物治疗阿片受体相关疾病的方法。进一步公开了两组式（I）的噻唑烷酮化合物：（i）每种化合物的对映体过量大于90%；（ii）每种化合物被氘取代。
• N2-(2-METHOXYPHENYL)PYRIMIDINE DERIVATIVE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION FOR CANCER PREVENTION OR TREATMENT CONTAINING SAME AS ACTIVE INGREDIENT
  申请人：KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

  公开号：US20180111905A1

  公开（公告）日：2018-04-26

  The present invention relates to a N2-(2-methoxyphenyl)pyrimidine derivative, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of cancer comprising the same as an active ingredient. The N2-(2-methoxyphenyl)pyrimidine derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention is very effective in suppressing anaplastic lymphoma kinase (ALK) activity and as a result it can improve the effectiveness of treatment on cancer cells having anaplastic lymphoma kinase (ALK) fusion proteins such as EML4-ALK and NPM-ALK, so that it can be effectively used as a pharmaceutical composition for preventing or treating cancer.

  本发明涉及一种N2-(2-甲氧基苯基)嘧啶衍生物，其制备方法，以及包含其作为活性成分的用于预防或治疗癌症的药物组合物。本发明的N2-(2-甲氧基苯基)嘧啶衍生物，其光学异构体，或其药学上可接受的盐对抑制间变性淋巴瘤激酶（ALK）活性非常有效，从而可以提高对具有间变性淋巴瘤激酶（ALK）融合蛋白如EML4-ALK和NPM-ALK的癌细胞的治疗效果，因此可以有效地用作预防或治疗癌症的药物组合物。
• [EN] IRAK4 INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS D'IRAK4 ET LEURS UTILISATIONS
  申请人：SYNBLIA THERAPEUTICS INC

  公开号：WO2019089422A1

  公开（公告）日：2019-05-09

  Compounds of Formula I as IRAK4 inhibitors are disclosed. The pharmaceutical compositions comprising compounds of formula I, methods of synthesis of these compounds, methods of treatment for diseases associated with IRAK-4 such as inflammatory diseases and autoimmune diseases using these compounds or compositions containing these compounds are also disclosed.

  公开了作为IRAK4抑制剂的I式化合物。还公开了包括I式化合物的药物组合物、这些化合物的合成方法、使用这些化合物或含有这些化合物的组合物进行治疗与IRAK-4相关的疾病，如炎症性疾病和自身免疫疾病的方法。
• 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。