N-(β-benzyloxycarbonylamino-α-hydroxypropionyloxy)succinimide | 75282-49-4

• 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: N-(β-benzyloxycarbonylamino-α-hydroxypropionyloxy)succinimide
• 英文别名: N-(R-β-benzyloxycarbonylamino-α-hydroxypropionyloxy)succinimide；(2,5-Dioxopyrrolidin-1-yl) 2-hydroxy-3-(phenylmethoxycarbonylamino)propanoate
• CAS: 75282-49-4
• 化学式: C₁₅H₁₆N₂O₇
• 分子量: 336.301
• InChiKey: IAYUSCSKPJJSDH-UHFFFAOYSA-N

物化性质

• 密度：
  1.45±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  24
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  122
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• 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
• 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。
• 2',3'-Dideoxy-2'-fluorokanamycin A and 1-N-(alpha-hydroxy-omega-aminoalkanoyl) derivatives thereof
  申请人：ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI

  公开号：EP0185323A2

  公开（公告）日：1986-06-25

  New compounds, 2',3'-dideoxy-2'-fluorokanamycin A and 1-N-(a-hydroxy-w-aminoalkanoyl) derivatives thereof, particularly 1-N-(DL- or L-3-amino-2-hydroxypropionyl)- and 1-N-(L-4-amino-2-hydroxybutyryt)-2',3'-dideoxy-2'-fluorokanamycins A are now provided, which are each useful as anti-bacterial agent. 2',3'-Dideoxy-2'-fluorokanamycin A is prepared by a process comprising condensing a 6-azido-4-0-protected-2,3-6-trideoxy-2-fluoro-a-D-ribo-hexopyranosyl bromide with the 4-hydroxyl group of a 6-0-(2',4',6'-tri-0- protected-3'-N-protected-3'-amino-3'-deoxy-α-D-glucopyranosyl)-1,3-bis-N-protected-2-deoxystreptamine, reducing the resulting condensation product to convert its azido group into an amino group, and removing the remaining amino-protecting and hydroxyl-protecting groups from the reduction product.

  现在提供了新的化合物，2',3'-二脱氧-2'-氟卡那霉素 A 及其 1-N-(a-羟基-w-氨基丙酰基)衍生物，特别是 1-N-(DL-或 L-3-氨基-2-羟基丙酰基)-和 1-N-(L-4-氨基-2-羟基丁酰)-2',3'-二脱氧-2'-氟卡那霉素 A，它们各自都是有用的抗菌剂。2',3'-双脱氧-2'-氟卡那霉素 A 的制备方法包括：将 6-叠氮-4-0-保护-2,3-6-三脱氧-2-氟-a-D-核 吡喃糖基溴化物与 6-0-(2',4',6'-三-0-保护-3'-N-保护-3'-氨基-3'-脱氧-α-D-吡喃葡萄糖基)-1.N-保护-3'-氨基-3'-脱氧-α-D-吡喃葡萄糖基)的 4-羟基缩合、3-双-N-保护-2-脱氧链霉胺，还原所得缩合产物，将其叠氮基团转化为氨基，并从还原产物中去除剩余的氨基保护基团和羟基保护基团。
• IMPROVED PROCESS FOR PREPARING ISEPAMICIN
  申请人：SCHERING CORPORATION

  公开号：EP0478707A1

  公开（公告）日：1992-04-08
• Improved process for preparing isepamicin
  申请人：SCHERING CORPORATION

  公开号：EP0405820B1

  公开（公告）日：1994-04-13