3-trifluoromethoxybenzyl azide | 620533-85-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 3-trifluoromethoxybenzyl azide
• 英文别名: 1-(Azidomethyl)-3-(trifluoromethoxy)benzene
• CAS: 620533-85-9
• 化学式: C₈H₆F₃N₃O
• 分子量: 217.15
• InChiKey: KGZGEQHTMIHHNC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  23.6
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  3-trifluoromethoxybenzyl azide 、 1-(4-乙炔基-2-甲氧基苯基)-4-甲基-1H-咪唑 在 copper(II) sulfate 、 sodium ascorbate 作用下， 以 乙醇 、 水 为溶剂， 生成 4-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl]-1-[3-(trifluoromethoxy)benzyl]-1H-1,2,3-triazole
  参考文献：
  名称：

  Triazoles as γ-secretase modulators

  摘要：

  Synthesis, SAR, and evaluation of aryl triazoles as novel gamma secretase modulators (GSMs) are presented in this communication. Starting from the literature and in-house leads, we evaluated a range of five-membered heterocycles as replacements for olefins commonly found in non-acid GSMs. 1,2,3-C-aryl-triazoles were identified as suitable replacements which exhibited good modulation of gamma-secretase activity, excellent pharmacokinetics and good central lowering of A beta 42 in Sprague-Dawley rats. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.04.089

文献信息

• ISOINDOLINE COMPOUND, AND PREPARATION METHOD, PHARMACEUTICAL COMPOSITION, AND APPLICATION OF ISOINDOLINE COMPOUND
  申请人：Shanghai Institute of Materia Medica, Chinese Academy of Sciences

  公开号：EP3896062A1

  公开（公告）日：2021-10-20

  The present invention relates to an isoindoline compound as represented by general formula (I) and used as a CRBN regulator, and a preparation method, a pharmaceutical composition, and an application of the isoindoline compound. Specifically, a class of polysubstituted isoindoline compound provided in the present invention, as a class of CRL4CRBN E3 ubiquitin ligase regulator having a novel structure, has good anti-tumor activity and immunoregulatory activity, and can be used for preparing drugs for treating diseases associated with a CRL4CRBN E3 ubiquitin ligase.

  本发明涉及一种由通式(I)表示并用作CRBN调节剂的异吲哚啉化合物，以及该异吲哚啉化合物的制备方法、药物组合物和应用。具体而言，本发明提供的一类多取代异吲哚啉化合物，作为一类结构新颖的CRL4CRBN E3泛素连接酶调节剂，具有良好的抗肿瘤活性和免疫调节活性，可用于制备治疗与CRL4CRBN E3泛素连接酶相关疾病的药物。
• TACHYKININ RECEPTOR ANTAGONISTS
  申请人：ELI LILLY AND COMPANY

  公开号：EP1501808B1

  公开（公告）日：2008-07-02
• TRIAZOLE DERIVATIVES AS TACHYKININ RECEPTOR ANTAGONISTS
  申请人：ELI LILLY AND COMPANY

  公开号：EP1501809B1

  公开（公告）日：2008-01-16