N_α-Boc-L-lysinol | 85535-54-2

• 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: N_α-Boc-L-lysinol
• 英文别名: tert-butyl (S)-(6-amino-1-hydroxyhexan-2-yl)carbamate；BOC-lysinol；N-BOC-L-Lysinol；tert-butyl N-[(2S)-6-amino-1-hydroxyhexan-2-yl]carbamate
• CAS: 85535-54-2
• 化学式: C₁₁H₂₄N₂O₃
• 分子量: 232.323
• InChiKey: HMYNSIWLDDOZIQ-VIFPVBQESA-N

物化性质

• 沸点：
  376.2±37.0 °C(Predicted)
• 密度：
  1.037±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  16
• 可旋转键数：
  8
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.91
• 拓扑面积：
  84.6
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  N_α-Boc-L-lysinol 生成 tert-butyl N-[(2S)-6-amino-1-oxohexan-2-yl]carbamate
  参考文献：
  名称：

  SIOIRI, TAKAYUKI;XAMADA, YASUMASA

  摘要：

  DOI：
• 作为产物：
  描述：

  NAlpha-BOC-Nε-FMOC-L-赖氨酸 在 sodium tetrahydroborate 、 三乙胺 作用下， 以 四氢呋喃 、 水 为溶剂， 生成 N_α-Boc-L-lysinol
  参考文献：
  名称：

  Exploration of the P1 SAR of aldehyde cathepsin K inhibitors

  摘要：

  The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S(1) subsite with a series of alpha-amino aldehyde derivatives substituted at the P(1) position afforded compounds with cathepsin K IC(50)s between 52 microM and 15 nM.

  DOI：

  10.1016/j.bmcl.2003.09.088

文献信息

• Synthesis of protected 3-aminopiperidine and 3-aminoazepane derivatives using enzyme cascades
  作者：Grayson J. Ford、Nico Kress、Ashley P. Mattey、Lorna J. Hepworth、Christopher R. Baldwin、James R. Marshall、Lisa S. Seibt、Min Huang、William R. Birmingham、Nicholas J. Turner、Sabine L. Flitsch

  DOI：10.1039/d0cc02976a

  日期：——

  Multi-enzyme cascades utilising variants of galactose oxidase and imine reductase led to the successful conversion of N-Cbz-protected L-ornithinol and L-lysinol to L-3-N-Cbz-aminopiperidine and L-3-N-Cbz-aminoazepane respectively, in up to 54% isolated yield. Streamlining the reactions into one-pot prevented potential racemisation of key labile intermediates and led to products with high enantiopurity

  利用半乳糖氧化酶和亚胺还原酶的变体的多酶级联反应成功地将N -Cbz保护的L-鸟氨酸和L-赖氨醇成功转化为L -3- N -Cbz-氨基哌啶和L -3- N -Cbz-氨基氮杂环庚烷分别获得高达54％的分离产率。将反应简化为一锅法可防止关键的不稳定中间体发生潜在的外消旋作用，并产生具有高对映体纯度的产品。
• ANTIBACTERIAL AMIDE MACROCYCLES IV
  申请人：Endermann Rainer

  公开号：US20080076745A1

  公开（公告）日：2008-03-27

  The invention relates to antibacterial amide macrocycles and processes for their preparation, their use for the treatment and/or prophylaxis of diseases and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially bacterial infections.

  该发明涉及抗菌酰胺大环化合物及其制备过程，其用于治疗和/或预防疾病以及用于制造治疗和/或预防疾病，特别是细菌感染的药物。
• ANTIBACTERIAL AMIDE-MACROCYCLES V
  申请人：ENDERMANN Rainer

  公开号：US20080275018A1

  公开（公告）日：2008-11-06

  The invention relates to antibacterial amide-macrocycles of formula (I), in which R 26 represents hydrogen, halogen, amino or methyl, R 7 represents a group of formula (II), (III), (IV) or (V), whereby R 1 represents hydrogen or hydroxy and * is the linkage site to the carbon atom, R 2 represents hydrogen or methyl and methods for their production, their use for the treatment and/or prophylaxis of diseases as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular of bacterial infections.

  本发明涉及式（I）的抗菌酰胺大环化合物，其中R26代表氢、卤素、氨基或甲基，R7代表式（II）、（III）、（IV）或（V）的基团，其中R1代表氢或羟基，*是连接到碳原子的连接位点，R2代表氢或甲基，以及它们的制备方法，它们用于治疗和/或预防疾病的用途，以及它们用于制备治疗和/或预防疾病的药物，特别是用于治疗细菌感染。
• Renin-inhibitory oligopeptides, their preparation and use
  申请人：SANKYO COMPANY LIMITED

  公开号：EP0228192A2

  公开（公告）日：1987-07-08

  Oligopeptides of formula (I): where R1R7 are various organic groups and n and m are 0 or 1, have renin-inhibitory activity and are particularly suitable for oral administration. They may be prepared by condensing their component amino acids or lower oligopeptides using conventional peptide synthesis reactions.

  式(I)的寡肽： 其中 R1R7 为各种有机基团，n 和 m 为 0 或 1，具有肾素抑制活性，特别适合口服。它们可以通过传统的肽合成反应缩合其氨基酸组分或低级寡肽来制备。
• Hydroxymorpholinone derivative and medicinal use thereof
  申请人：Nakamura Masayuki

  公开号：US20050176704A1

  公开（公告）日：2005-08-11

  A compound represented by the following formula (I) wherein R 1 and R 2 are each a lower alkyl group optionally having substituents, which has a calpain inhibitory activity, or a salt thereof is provided.

  下式(I)代表的化合物 其中 R 1 和 R 2 均为可选具有取代基的低级烷基，具有钙蛋白酶抑制活性的化合物或其盐。