L-(-)-α-hydroxy-δ-carbobenzoxyaminovaleric acid | 227197-74-2

• 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: L-(-)-α-hydroxy-δ-carbobenzoxyaminovaleric acid
• 英文别名: 5-{[(Benzyloxy)carbonyl]amino}-2-hydroxypentanoic acid；2-hydroxy-5-(phenylmethoxycarbonylamino)pentanoic acid
• CAS: 227197-74-2
• 化学式: C₁₃H₁₇NO₅
• 分子量: 267.282
• InChiKey: VJDLMVOJNLCDRU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  19
• 可旋转键数：
  8
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  95.9
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  5-amino-2-hydroxypentanoic acid 、 氯甲酸苄酯 以 水 为溶剂， 以82.5%的产率得到L-(-)-α-hydroxy-δ-carbobenzoxyaminovaleric acid
  参考文献：
  名称：

  Derivatives of an antibiotic XK-62-2 and the process for the production

  摘要：

  通过对抗生素XK-62-2进行化学修饰，产生了新的衍生物。这些新的衍生物是1-N-(α-羟基-δ-氨基戊酰基)XK-62-2和1-N-(α-羟基-ε-氨基癸酰基)XK-62-2，以及它们的酸加成盐。

  公开号：

  US04076931A1

文献信息

• Phosphonic acid derivative having inhibitory activity against carboxypeptidase B
  申请人：Meiji Seika Kaisha Ltd.

  公开号：US20030119787A1

  公开（公告）日：2003-06-26

  A compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof: 1 wherein R 1 represents hydrogen atom, an alkyl group, a substituted alkyl group and the like; R 2 and R 3 represent hydrogen atom, an alkyl group, a substituted alkyl group, an alkoxyl group and the like; X represents —CH 2 —, —O—, or —NH—; A represents the following group (II): 2 [in which R 7 and R 8 represent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group and the like; R 9 and R 10 represents hydrogen atom, a halogen atom, hydroxyl group, phenyl group, an alkyl group and the like] and the like; and E represents hydrogen atom and the like, which has inhibitory activity against carboxypeptidase B and is useful for therapeutic and/or preventive treatment of a thrombotic disease.

  以下是通用式（I）及其药学上可接受的盐所代表的化合物：其中R1代表氢原子、烷基、取代烷基等；R2和R3代表氢原子、烷基、取代烷基、烷氧基等；X代表—CH2—、—O—或—NH—；A代表以下基团（II）：其中R7和R8代表氢原子、烷基、酰基、烷氧羰基等；R9和R10代表氢原子、卤素原子、羟基、苯基、烷基等；E代表氢原子等，具有对羧肽酶B的抑制活性，可用于治疗和/或预防血栓性疾病。
• NOVEL AMINOGLYCOSIDE ANTIBIOTICS
  申请人：Kobayashi Yoshihiko

  公开号：US20120165283A1

  公开（公告）日：2012-06-28

  This invention relates to novel aminoglycoside antibiotics, which have potent antimicrobial activity against bacteria, which induce infectious diseases, particularly MRSA, and has no significant nephrotoxicity, and process for producing them. More particularly, the present invention relates to compounds represented by formula (Ia) or their pharmacologically acceptable salts or solvates, or their diastereomer mixtures, antimicrobial agents comprising them, and a process for producing them.

  这项发明涉及一种新型氨基糖苷类抗生素，对引起感染性疾病的细菌，特别是MRSA具有强效的抗菌活性，并且没有显著的肾毒性，并提供制备它们的方法。更具体地，本发明涉及由式（Ia）表示的化合物或其药理学上可接受的盐或溶剂合物，或其对映体混合物，包括它们的抗微生物剂以及制备它们的方法。
• Novel aminoglycoside antibiotics
  申请人：Kobayashi Yoshihiko

  公开号：US20090186841A1

  公开（公告）日：2009-07-23

  This invention relates to novel aminoglycoside antibiotics, which have potent antimicrobial activity against bacteria, which induce infectious diseases, particularly MRSA, and has no significant nephrotoxicity, and process for producing them. More particularly, the present invention relates to compounds represented by formula (Ia) or their pharmacologically acceptable salts or solvates, or their diastereomer mixtures, antimicrobial agents comprising them, and a process for producing them.

  本发明涉及一种新型氨基糖苷类抗生素，对引起传染病的细菌，特别是MRSA具有强效的抗微生物活性，并且没有显著的肾毒性，并提供了其生产方法。更具体地说，本发明涉及由式（Ia）表示的化合物或其药理学上可接受的盐或溶剂或其对映体混合物，包含它们的抗微生物剂以及生产它们的方法。
• 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
• PHOSPHONIC ACID DERIVATIVES HAVING CARBOXYPEPTIDASE B INHIBITORY ACTIVITY
  申请人：Meiji Seika Kaisha, Ltd.

  公开号：EP1152004A1

  公开（公告）日：2001-11-07

  A compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof: wherein R1 represents hydrogen atom, an alkyl group, a substituted alkyl group and the like; R2 and R3 represent hydrogen atom, an alkyl group, a substituted alkyl group, an alkoxyl group and the like; X represents -CH2-, -O-, or -NH-; A represents the following group (II): [in which R7 and R8 represent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group and the like; R9 and R10 represents hydrogen atom, a halogen atom, hydroxyl group, phenyl group, an alkyl group and the like] and the like; and E represents hydrogen atom and the like, which has inhibitory activity against carboxypeptidase B and is useful for therapeutic and/or preventive treatment of a thrombotic disease.

  由以下通式（I）代表的化合物及其药理学上可接受的盐： 其中 R1 代表氢原子、烷基、取代的烷基等；R2 和 R3 代表氢原子、烷基、取代的烷基、烷氧基等；X 代表 -CH2-、-O- 或 -NH-；A 代表以下基团 (II)： [其中 R7 和 R8 代表氢原子、烷基、酰基、烷氧基羰基等；R9 和 R10 代表氢原子、卤素原子、羟基、苯基、烷基等]等；E 代表氢原子等，对羧肽酶 B 具有抑制活性，可用于血栓性疾病的治疗和/或预防。