4-[2-[2-(2-叠氮乙氧基)乙氧基]乙氧基]苯胺 | 1402230-95-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 中文名称: 4-[2-[2-(2-叠氮乙氧基)乙氧基]乙氧基]苯胺
• 英文名称: 4-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]aniline
• CAS: 1402230-95-8
• 化学式: C₁₂H₁₈N₄O₃
• 分子量: 266.3
• InChiKey: JFVOSMASAOMDAZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  19
• 可旋转键数：
  10
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  68.1
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  (5Z)-5-benzylidene-2-ethylsulfanyl-3,5-dihydroimidazol-4-one 、 4-[2-[2-(2-叠氮乙氧基)乙氧基]乙氧基]苯胺 在 sodium acetate 作用下， 以11.3 mg的产率得到(5Z)-2-[4-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]anilino]-4-benzylidene-3,5-dihydroimidazol-5-one
  参考文献：
  名称：

  Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines

  摘要：

  Leucettines, a family of marine sponge-derived 2-aminoimidazolone alkaloids, are potent inhibitors of DYRKs (dual-specificity, tyrosine phosphoiylation regulated kinases) and CLKs (cdc2-like kinases). They constitute promising pharmacological leads for the treatment of several diseases, including Alzheimer's disease and Down syndrome. In order to investigate the scope of potential targets of Leucettine L41, a representative member of the chemical class, we designed an affinity chromatography strategy based on agarose-immobilized leucettines. A synthesis protocol for the attachment of a polyethylene (3 or 4 units) linker to L41 was first established. The linker attachment site on L41 was selected on the basis of the co-crystal structure of L41 with several kinases. L41 was then covalently bound to agarose beads through the primary amine located at the end of the linker. Control, kinase inactive Leucettine was also immobilized, as well as free linker devoid of ligand. Extracts of several mouse tissues revealed a complex pattern of interacting proteins, some of which probably resulting from non-specific, hydrophobic binding, while others representing bona fide Leucettine-interacting proteins. DYRK1A and GSK-3 (glycogen synthase kinase-3) were confirmed as interacting targets by Western blotting in various mouse tissues. The Leucettine affinity chromatography resin constitutes a powerful tool to purify and identify the targets of this new promising therapeutic class of molecules. (C) 2013 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2013.01.035
• 作为产物：
  描述：

  2-[2-[2-[4-(tert-butoxycarbonylamino)phenoxy]ethoxy]ethoxy]ethyl-4-methylbenzenesulfonate 在 sodium azide 作用下， 以 乙醇 、 水 为溶剂， 反应 1.0h， 生成 4-[2-[2-(2-叠氮乙氧基)乙氧基]乙氧基]苯胺
  参考文献：
  名称：

  Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines

  摘要：

  Leucettines, a family of marine sponge-derived 2-aminoimidazolone alkaloids, are potent inhibitors of DYRKs (dual-specificity, tyrosine phosphoiylation regulated kinases) and CLKs (cdc2-like kinases). They constitute promising pharmacological leads for the treatment of several diseases, including Alzheimer's disease and Down syndrome. In order to investigate the scope of potential targets of Leucettine L41, a representative member of the chemical class, we designed an affinity chromatography strategy based on agarose-immobilized leucettines. A synthesis protocol for the attachment of a polyethylene (3 or 4 units) linker to L41 was first established. The linker attachment site on L41 was selected on the basis of the co-crystal structure of L41 with several kinases. L41 was then covalently bound to agarose beads through the primary amine located at the end of the linker. Control, kinase inactive Leucettine was also immobilized, as well as free linker devoid of ligand. Extracts of several mouse tissues revealed a complex pattern of interacting proteins, some of which probably resulting from non-specific, hydrophobic binding, while others representing bona fide Leucettine-interacting proteins. DYRK1A and GSK-3 (glycogen synthase kinase-3) were confirmed as interacting targets by Western blotting in various mouse tissues. The Leucettine affinity chromatography resin constitutes a powerful tool to purify and identify the targets of this new promising therapeutic class of molecules. (C) 2013 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2013.01.035

文献信息

• [EN] HETEROARYL COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS HÉTÉROARYLE ET UTILISATIONS ASSOCIÉES
  申请人：AVILA THERAPEUTICS INC

  公开号：WO2011090760A1

  公开（公告）日：2011-07-28

  The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

  本发明提供了化合物，其药物学上可接受的组成物以及使用它们的方法。
• HETEROARYL COMPOUNDS AND USES THEREOF
  申请人：Singh Juswinder

  公开号：US20100249092A1

  公开（公告）日：2010-09-30

  The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

  本发明提供化合物及其药学上可接受的组成物，以及使用它们的方法。
• SYNTHESIS OF HYBRID BLOCK COPOLYMERS AND USES THEREOF
  申请人：Breitenkamp Kurt

  公开号：US20110021718A1

  公开（公告）日：2011-01-27

  The present invention relates to the field of polymer chemistry and more particularly to multiblock copolymers and methods of preparing the same.
• US7601796B2
  申请人：——

  公开号：US7601796B2

  公开（公告）日：2009-10-13
• US8268936B2
  申请人：——

  公开号：US8268936B2

  公开（公告）日：2012-09-18