2-(3-Amino-5-benzo[1,3]dioxol-5-yl-2-oxo-2,3-dihydro-benzo[e][1,4]diazepin-1-yl)-acetamide | 724422-65-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯二氮卓类
• 英文名称: 2-(3-Amino-5-benzo[1,3]dioxol-5-yl-2-oxo-2,3-dihydro-benzo[e][1,4]diazepin-1-yl)-acetamide
• CAS: 724422-65-5
• 化学式: C₁₈H₁₆N₄O₄
• 分子量: 352.349
• InChiKey: SZYHOORGXQHDAC-UHFFFAOYSA-N

反应信息

• 作为反应物：
  描述：

  2-(S)-methyl-3-(3,4-difluorophenyl)propionic acid 、 2-(3-Amino-5-benzo[1,3]dioxol-5-yl-2-oxo-2,3-dihydro-benzo[e][1,4]diazepin-1-yl)-acetamide 在 1-羟基苯并三唑 、 1-(3-二甲基氨基丙基)-3-乙基碳二亚胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以70%的产率得到(S)-N-((S)-5-Benzo[1,3]dioxol-5-yl-1-carbamoylmethyl-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-3-(3,4-difluoro-phenyl)-2-methyl-propionamide
  参考文献：
  名称：

  High affinity, bioavailable 3-Amino-1,4-benzodiazepine-Based γ-Secretase inhibitors

  摘要：

  In this paper, we describe the development of a novel series of high affinity, orally bioavailable 3-amino-1,4 benzodiazepine-based gamma-secretase inhibitors for the potential treatment of Alzheimer's disease. We disclose structure-activity relationships based around the 1, 3 and 5 positions of the benzodiazepine core structure. (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2003.07.031
• 作为产物：
  描述：

  (5-Benzo[1,3]dioxol-5-yl-1-carbamoylmethyl-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-carbamic acid benzyl ester 在 氢溴酸 、 溶剂黄146 作用下， 生成 2-(3-Amino-5-benzo[1,3]dioxol-5-yl-2-oxo-2,3-dihydro-benzo[e][1,4]diazepin-1-yl)-acetamide
  参考文献：
  名称：

  High affinity, bioavailable 3-Amino-1,4-benzodiazepine-Based γ-Secretase inhibitors

  摘要：

  In this paper, we describe the development of a novel series of high affinity, orally bioavailable 3-amino-1,4 benzodiazepine-based gamma-secretase inhibitors for the potential treatment of Alzheimer's disease. We disclose structure-activity relationships based around the 1, 3 and 5 positions of the benzodiazepine core structure. (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2003.07.031