(R)-2-Ethyl-aziridine-1-carboxylic acid tert-butyl ester | 197020-61-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂环丙烷
• 英文名称: (R)-2-Ethyl-aziridine-1-carboxylic acid tert-butyl ester
• 英文别名: 1,1-Dimethylethyl (2R)-2-ethyl-1-aziridinecarboxylate；tert-butyl (2R)-2-ethylaziridine-1-carboxylate
• CAS: 197020-61-4
• 化学式: C₉H₁₇NO₂
• 分子量: 171.239
• InChiKey: DEXAOHLCGKXLGS-PVSHWOEXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  29.3
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  N-Boc-(R)-(+)-2-氨基-1-丁醇 在 氢氧化钾 、 对甲苯磺酰氯 作用下， 以 乙醚 为溶剂， 反应 4.0h， 以72%的产率得到(R)-2-Ethyl-aziridine-1-carboxylic acid tert-butyl ester
  参考文献：
  名称：

  A Convenient One-Pot Conversion of N-Boc-β-Aminoalcohols into N-Boc-Aziridines

  摘要：

  本文描述了一种高效的一步转化法，将手性N-保护的β-氨基醇转化为相应的氮丙啶。

  DOI：

  10.1055/s-1997-940

文献信息

• MACROCYCLIC BETA-SECRETASE INHIBITORS
  申请人：Stamford Andrew W.

  公开号：US20100178294A1

  公开（公告）日：2010-07-15

  Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 , R 2 , R 3 , n and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
• SUBSTITUTED AMIDE BETA SECRETASE INHIBITORS
  申请人：Huang Ying

  公开号：US20110003825A1

  公开（公告）日：2011-01-06

  Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 , R 2 , R 3 , R 4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
• US8012953B2
  申请人：——

  公开号：US8012953B2

  公开（公告）日：2011-09-06
• US8367712B2
  申请人：——

  公开号：US8367712B2

  公开（公告）日：2013-02-05
• A Convenient One-Pot Conversion of N-Boc-<i>β</i>-Aminoalcohols into N-Boc-Aziridines
  作者：Pablo Wessig、Jutta Schwarz

  DOI：10.1055/s-1997-940

  日期：1997.8

  This paper describes an efficient single step transformation of chiral N-protected β-amino alcohols into appropriate aziridines.

  本文描述了一种高效的一步转化法，将手性N-保护的β-氨基醇转化为相应的氮丙啶。