4-N-benzyloxycarbonyl-L-4-amino-2-hydroxybutyric acid N-hydroxysuccinimide ester | 77397-99-0

• 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
• 英文名称: 4-N-benzyloxycarbonyl-L-4-amino-2-hydroxybutyric acid N-hydroxysuccinimide ester
• 英文别名: L-(-)-γ-benzyloxycarbonylamino-α-hydroxybutyric acid N-hydroxysuccinimide ester；N-(γ-benzyloxycarbonylamino-α-hydroxybutyryloxy)succinimide；N-(R-γ-benzyloxycarbonylamino-α-hydroxybutyryloxy)succinimide；N-(RS-γ-benzyloxycarbonylamino-α-hydroxybutyryloxy)succinimide；(2,5-Dioxopyrrolidin-1-yl) 2-hydroxy-4-(phenylmethoxycarbonylamino)butanoate
• CAS: 77397-99-0
• 化学式: C₁₆H₁₈N₂O₇
• 分子量: 350.328
• InChiKey: GXUXZODCJQNXBE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  25
• 可旋转键数：
  9
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.375
• 拓扑面积：
  122
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• Aminoglycosides as antibiotics
  申请人：Haddad Jalal

  公开号：US20050171035A1

  公开（公告）日：2005-08-04

  The present invention provides aminoglycosides and pharmaceutical compositions that include the aminoglycosides. The aminogylcosides are useful to treat or prevent infectious diseases (e.g., bacterial infections) in a mammal (e.g., human).

  本发明提供了氨基糖苷类化合物和包含该氨基糖苷类化合物的药物组合物。该氨基糖苷类化合物可用于治疗或预防哺乳动物（如人）的传染病（例如细菌感染）。
• AMINOGLYCOSIDES AS ANTIBIOTICS
  申请人：Haddad Jalal

  公开号：US20070203081A1

  公开（公告）日：2007-08-30

  The present invention provides aminoglycosides and pharmaceutical compositions that include the aminoglycosides. The aminoglycosides are useful to treat or prevent infectious diseases (e.g., bacterial infections) in a mammal (e.g., human).

  本发明提供了氨基糖苷和包括氨基糖苷的制药组合物。氨基糖苷可用于治疗或预防哺乳动物（如人类）的感染性疾病（如细菌感染）。
• Process for preparing aminoglycoside derivatives, novel derivatives obtained and pharmaceutical compositions containing such derivatives
  申请人：Technobiotic Ltd.

  公开号：EP0000473A1

  公开（公告）日：1979-02-07

  This invention relates to a process for preparing 2'-hydroxy- 2'-desamino-4,6-di-0-(aminoglycosyl) -1,3-diaminocyclitols having a 6'-amino function and pharmaceutically acceptable acid addition salts thereof, to novel compounds and salts obtained by this process; and to novel antibacterially active compositions comprising such novel compounds or salts. The process comprises reacting the corresponding N-protected (except the 2'-amino)-4,6- di-0- (aminoglycosyl)-1,3-diaminocyclitol with hydrogen peroxide in the presence of tungstate ion, followed by cleavage of the thereby formed 2'-oximino derivative and by reduction of the resulting 2'-oxo derivative and by removal of the N-protecting groups. The preferred group of novel compounds obtained by this process are the 1-N- (ω-amino-α- hydroxyalkanoyl) -2'-hydroxy-2'- desamino-4,6-di-0- (aminoglycosyl)- 1,3-diaminocyclitols. The compounds obtained by the process of !this invention exhibit antibacterial activity

  本发明涉及一种制备具有 6'-氨基功能的 2'-羟基-2'-二氨基-4,6-二-0-(氨基糖基)-1,3-二氨基环糖醇及其药学上可接受的酸加成盐的工艺，涉及通过该工艺获得的新型化合物和盐；还涉及包含这种新型化合物或盐的新型抗菌活性组合物。 该工艺包括在钨酸盐离子存在下，使相应的 N-保护（2'-氨基除外）-4,6-二-0-（氨基糖基）-1,3-二氨基环糖醇与过氧化氢反应，然后裂解由此形成的 2'-氧亚氨基衍生物，还原生成的 2'-氧代衍生物，并除去 N-保护基团。 通过该工艺获得的新型化合物的优选类别是 1-N-（ω-氨基-α-羟基烷酰基）-2'-羟基-2'-去氨基-4,6-二-0-（氨基糖基）-1,3-二氨基环糖醇。通过本发明工艺获得的化合物具有抗菌活性
• 1-N-acylated and 1-N-alkylated derivatives of 4-0-substituted -2-deoxystreptamine aminoglycosides
  申请人：ELI LILLY AND COMPANY

  公开号：EP0048614A1

  公开（公告）日：1982-03-31

  Novel 1-N-acylated or 1-N-alkylated derivatives of a 4-O-substituted-2-deoxystreptamine aminoglycoside selected from the group consisting of; apramycin, a or β-(C1 to C6 alkyl)aprosaminide, a or β-(C2 to C6 hydroxyalkyl)aprosaminide, a or β-(C2 to C6 aminoalkyl)aprosaminide, a or β-(C2 to C6 protected aminoalkyl) aprosaminide, a or β-(C3 to C6 aminohydroxyalkyl)-aprosaminide, a or β-(C3 to C6 (protected amino)hydroxyalkyl)aprosaminide, and pharmaceutically-acceptable acid addition salts thereof are disclosed. They are useful for treating warm blooded animals suffering from bacterial diseases. They and 1-N-acylated and 1-N-alkylated derivatives of lividamine, paromamine and the 6'-N-protected derivatives of nebramine, neamine, gentamine C1, gentamine C1a, gentamine C2, gentamine C2a, and gentamine C2b, and pharmaceutically-acceptable acid addition salts thereof can be prepared by reacting the corresponding aminoglycoside substrate with a zinc salt Zn (X2), X being C, to C10 carboxylate, in water, diluting with a polar organic solvent, treating with an alkalating agent or acylating agent, optionally, deprotecting the amino or N-protected substituents, optionally, reducing carbonyl portions of an acyl group, and recovering as a free base or as a pharmaceutically-acceptable acid addition salt.

  选自以下组别的 4-O-取代的-2-脱氧链霉胺氨基糖苷的 1-N-酰化或 1-N-烷化的新型衍生物； 阿普霉素 或 β-(C1-C6烷基)阿朴酰胺、 或 β-(C2-C6羟烷基)阿朴沙明、 或 β-(C2 至 C6 氨基烷基)阿朴沙明、 或 β-(C2 至 C6 受保护氨基烷基)阿朴沙明内酯，a 或 或 β-(C3 至 C6 氨基羟烷基)-槟榔甙，一种或 β-(C3 至 C6 (受保护氨基)羟烷基)槟榔甙，以及 及其药学上可接受的酸加成盐。它们可用于 治疗患有细菌性疾病的温血动物。通过将相应的氨基糖苷底物与锌盐 Zn (X2)反应，可制备它们和利维胺、扑尔敏的 1-N- 乙酰化和 1-N- 烷基化衍生物，以及奈布拉明、奈胺、龙胆胺 C1、龙胆胺 C1a、龙胆胺 C2、龙胆胺 C2a 和龙胆胺 C2b 的 6'-N 保护衍生物及其药学上可接受的酸加成盐、X 是 C 至 C10 羧酸盐，在水中反应，用极性有机溶剂稀释，用碱化剂或酰化剂处理，可选地对氨基或 N 保护取代基进行脱保护，可选地对酰基的羰基部分进行还原，然后以游离碱或药学上可接受的酸加成盐的形式回收。
• 1N-(omega-amino-alpha-hydroxyalkanoyl)-2',3'-dideoxykanamycin A and the production of the same
  申请人：ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI

  公开号：EP0139553A2

  公开（公告）日：1985-05-02

  1-N-(L-3-amino-2-hydroxypropionyl)-2',3'-dideoxykanamycin A and 1-N-(L-4-amino-2-hydroxybutyryl)-2',3'- dideoxykanamycin A are now provided which each is a new compound useful as antibacterial agent. The new compounds each is produced by acylating the 1-amino group of 2',3'-dideoxykanamycin A with L-3-amino-2-hydroxypropionic or L-4-amino-2-hydroxybutyric acid.

  现在提供的 1-N-(L-3-氨基-2-羟基丙酰基)-2',3'-二脱氧卡那霉素 A 和 1-N-(L-4-氨基-2-羟基丁酰基)-2',3'-二脱氧卡那霉素 A 都是一种可用作抗菌剂的新化合物。 这些新化合物都是通过将 2',3'-二脱氧卡那霉素 A 的 1-氨基与 L-3- 氨基-2-羟基丙酸或 L-4- 氨基-2-羟基丁酸酰化而制得的。