methyl (RS)-2-amino-3-phenyl-2-aminomethylpropanoate | 134915-83-6

• 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: methyl (RS)-2-amino-3-phenyl-2-aminomethylpropanoate
• 英文别名: methyl 2,3-Diamino-2-phenylmethylpropionate；Methyl 2-amino-2-(aminomethyl)-3-phenylpropanoate
• CAS: 134915-83-6
• 化学式: C₁₁H₁₆N₂O₂
• 分子量: 208.26
• InChiKey: KZAGXUHMMCNIKT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  15
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  78.3
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  methyl (RS)-2-amino-3-phenyl-2-aminomethylpropanoate 、 1-[(S)-2-Benzyloxycarbonylamino-3-(1H-indol-3-yl)-1-methylsulfanyl-propylidene]-piperidinium; iodide 以 甲醇 为溶剂， 生成 methyl 5-benzyl-2-[2-(1H-indol-3-yl)-1-(phenylmethoxycarbonylamino)ethyl]-1,4-dihydroimidazole-5-carboxylate
  参考文献：
  名称：

  咪唑啉作为酰胺键的替代物

  摘要：

  这项工作描述了2,5,5-三取代的咪唑啉作为酰胺键替代物的用途。该替代物被掺入到Phe，Trp，Lys和Nle的二肽衍生物中，并且还被掺入CCK-4类似物Trp-Nle-Asp-Phe-NH 2和五肽胃泌素类似物Gly-Trp-Nle-Asp-Phe-NH 2中。酰胺键置换以对映体和非对映体纯的形式合成。

  DOI：

  10.1016/0040-4020(95)00273-b
• 作为产物：
  描述：

  methyl 2-(4-chlorobenzylidene)amino-3-phenylpropionate 在 一水合肼 作用下， 以 甲醇 为溶剂， 反应 2.0h， 生成 methyl (RS)-2-amino-3-phenyl-2-aminomethylpropanoate
  参考文献：
  名称：

  Amide bond replacements : incorporation of a 2,5,5-trisubstituted imidazoline into dipeptides and into a CCK-4 derivative.

  摘要：

  Synthetic methodology for the introduction of a 2,5,5-trisubstituted imidazoline ring as an amide replacement into dipeptide derivatives of Phe, Trp, Lys (N-epsilon-CBZ) and Nle is described. This replacement is also incorporated into the Trp-Nle bond of the tetrapeptide CCK-4 derivative Trp-Nle-Asp-Phe-NH2 and the pentagastrin derivative Gly-Trp-Nle-Asp-Phe-NH2.

  DOI：

  10.1016/s0040-4039(00)79701-2

文献信息

• Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting &bgr;-amyloid peptide release and/or its synthesis by use of such compounds
  申请人：Athena Neurosciences, Inc.

  公开号：US06506782B1

  公开（公告）日：2003-01-14

  Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

  公开了抑制β-淀粉样肽释放和/或其合成的化合物，因此可用于治疗阿尔茨海默病。还公开了包含抑制β-淀粉样肽释放和/或其合成的化合物的药物组合物，以及使用这些药物组合物预防性和治疗性地治疗阿尔茨海默病的方法。
• Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
  申请人：——

  公开号：US20030130188A1

  公开（公告）日：2003-07-10

  Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

  本发明揭示了一些化合物，可以抑制&bgr;-淀粉样肽的释放和/或合成，因此在治疗阿尔茨海默病方面具有实用性。本发明还揭示了包含抑制&bgr;-淀粉样肽释放和/或合成的化合物的制药组合物，以及使用这些制药组合物预防和治疗阿尔茨海默病的方法。
• HETEROCYCLIC COMPOUNDS AND THEIR USE FOR INHIBITING $g(b)-AMYLOID PEPTIDE
  申请人：Elan Pharmaceuticals, Inc.

  公开号：EP0968198A1

  公开（公告）日：2000-01-05
• US6506782B1
  申请人：——

  公开号：US6506782B1

  公开（公告）日：2003-01-14
• US6849650B2
  申请人：——

  公开号：US6849650B2

  公开（公告）日：2005-02-01