2-aminoethyl 3,4,6-tri-O-acetyl-2-(acetylamino)-2-deoxy-β-D-glucopyranoside | 64448-37-9

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-aminoethyl 3,4,6-tri-O-acetyl-2-(acetylamino)-2-deoxy-β-D-glucopyranoside
• 英文别名: (2-aminoethyl)-2-acetamido-3,4,5-tri-O-acetyl-2-deoxy-β-D-glucopyranoside；2-aminoethyl 3,4,6-tri-O-acetyl-2-(acetylamino)-2-deoxy-beta-D-glucopyranoside；[(2R,3S,4R,5R,6R)-5-acetamido-3,4-diacetyloxy-6-(2-aminoethoxy)oxan-2-yl]methyl acetate
• CAS: 64448-37-9
• 化学式: C₁₆H₂₆N₂O₉
• 分子量: 390.39
• InChiKey: PWFLODWGSOYBGC-OXGONZEZSA-N

物化性质

• 沸点：
  563.9±50.0 °C(Predicted)
• 密度：
  1.27±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -1.8
• 重原子数：
  27
• 可旋转键数：
  11
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  153
• 氢给体数：
  2
• 氢受体数：
  10

反应信息

• 作为反应物：
  描述：

  2-aminoethyl 3,4,6-tri-O-acetyl-2-(acetylamino)-2-deoxy-β-D-glucopyranoside 、 2-喹喔啉羧酸 在 sodium methylate 、 N,N'-二环己基碳二亚胺 作用下， 生成
  参考文献：
  名称：

  Communication: Synthesis of a Library of β-GlcNAc Glycosides to Screen for Efficient in Vivo Glycosyltransferase Acceptors

  摘要：

  DOI：

  10.1080/07328309908544011
• 作为产物：
  描述：

  2-azidoethyl 2-acetamido-3,4,6-tri-O-acetyl-2-deoxy-β-D-glucopyranoside 在 palladium on activated charcoal 氢气 作用下， 以 甲醇 、 溶剂黄146 为溶剂， 反应 24.0h， 以35%的产率得到2-aminoethyl 3,4,6-tri-O-acetyl-2-(acetylamino)-2-deoxy-β-D-glucopyranoside
  参考文献：
  名称：

  Site-selective depurination by a periodate-dependent deoxyribozyme

  摘要：

  一种脱氧核酶被鉴定为能够介导其5′-末端鸟苷酸的位点选择性去嘌呤化，使用过氧酸根离子（IO4–）作为必需的辅因子。

  DOI：

  10.1039/b704507g

文献信息

• GLUCOSE-RESPONSIVE INSULIN CONJUGATES
  申请人：Merck Sharp & Dohme Corp.

  公开号：US20150105317A1

  公开（公告）日：2015-04-16

  Insulin conjugates comprising an insulin molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein the saccharide for at least one ligand of the linker is fucose are disclosed. The insulin conjugates display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.

  本发明涉及胰岛素共轭物，包括将胰岛素分子共价连接至至少一个双齿配体的连接物中，每个配体独立连接到包含一种含糖和其中至少一个连接物的配体的糖类，其中连接物的至少一个配体的糖类为岩藻糖。这些胰岛素共轭物展示出对系统浓度的糖类（如葡萄糖或α-甲基甘露糖）具有响应的药代动力学（PK）和/或药效动力学（PD）特性，即使在给予需要的受试者时，也不需要外源多价糖类结合分子（如Con A）。
• [EN] GLUCOSE-RESPONSIVE INSULIN CONJUGATES<br/>[FR] CONJUGUÉS D'INSULINE SENSIBLES AU GLUCOSE
  申请人：MERCK SHARP & DOHME

  公开号：WO2016164288A1

  公开（公告）日：2016-10-13

  Insulin conjugates comprising an insulin analog molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein the saccharide for at least one ligand of the linker is fucose are disclosed. The insulin conjugates display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.

  包含胰岛素类似物分子的胰岛素共轭物，与至少一个双齿配体连接物共价连接，每个配体独立连接到一个含有糖类的配体，并且连接物中至少一个配体的糖类是富马醇。这些胰岛素共轭物显示出对糖类（如葡萄糖或α-甲基甘露糖）的体内浓度响应的药代动力学（PK）和/或药效动力学（PD）特性，即使在向需要者施用时，也无需外源多价糖类结合分子（如Con A）。
• GLYCO-MODIFIED ATRIAL NATRIURETIC PEPTIDE
  申请人：Daiichi Sankyo Company, Limited

  公开号：US20160017015A1

  公开（公告）日：2016-01-21

  The present invention provides a modified atrial natriuretic peptide that exhibits prolonged duration in blood and maintains cGMP elevating activity. The present invention provides a modified peptide in which at least one sugar substance is linked directly through a glycosidic bond or via a linker structure to at least one hANP peptide, or a pharmaceutically acceptable salt thereof, a medicament comprising the modified peptide or the salt thereof as an active ingredient, etc.

  本发明提供一种经过改良的心房利钠肽，其在血液中表现出持续时间较长，并保持cGMP升高活性。本发明提供一种改良的肽，其中至少一个糖物质通过糖苷键或通过连接物结构直接连接到至少一个hANP肽，或其药学上可接受的盐，以及包含所述改良肽或其盐作为活性成分的药物等。
• Glucose-responsive insulin conjugates
  申请人：Merck Sharp & Dohme Corp.

  公开号：US09427475B2

  公开（公告）日：2016-08-30

  Insulin conjugates comprising an insulin molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein the saccharide for at least one ligand of the linker is fucose are disclosed. The insulin conjugates display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.

  本发明公开了胰岛素共轭物，包括一个胰岛素分子与至少一个双叉联接物共价结合，该联接物具有两个臂，每个臂独立地连接到一个配体，该配体包括一个糖和至少一个联接物的糖苷，其中至少一个联接物的糖苷为岩藻糖。即使在没有外源多价糖结合分子（如Con A）的情况下，这些胰岛素共轭物显示出对系统浓度的糖类（如葡萄糖或α-甲基甘露糖）的药代动力学（PK）和/或药效学（PD）特性的响应，即当其被用于需要该物质的患者时。
• Glyco-modified atrial natriuretic peptide
  申请人：Daiichi Sankyo Company, Limited

  公开号：US10947289B2

  公开（公告）日：2021-03-16

  The present invention provides a modified atrial natriuretic peptide that exhibits prolonged duration in blood and maintains cGMP elevating activity. The present invention provides a modified peptide in which at least one sugar substance is linked directly through a glycosidic bond or via a linker structure to at least one hANP peptide, or a pharmaceutically acceptable salt thereof, a medicament comprising the modified peptide or the salt thereof as an active ingredient, etc.

  本发明提供了一种经修饰的心房利钠肽，它在血液中的持续时间长，并保持 cGMP 升高活性。本发明提供了一种修饰肽，其中至少有一种糖类物质直接通过糖苷键或通过连接体结构与至少一种 hANP 肽连接，或其药学上可接受的盐；一种包含该修饰肽或其盐作为活性成分的药物等。