(3-methyl-2-(morpholin-4-yl)-5-nitrophenyl)methanamine hydrochloride | 1312290-97-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: (3-methyl-2-(morpholin-4-yl)-5-nitrophenyl)methanamine hydrochloride
• 英文别名: [3-Methyl-2-(morpholin-4-yl)-5-nitrophenyl]methanamine hydrochloride；(3-methyl-2-morpholin-4-yl-5-nitrophenyl)methanamine;hydrochloride
• CAS: 1312290-97-3
• 化学式: C₁₂H₁₇N₃O₃*ClH
• 分子量: 287.746
• InChiKey: UAGZKSCENIFZJG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.62
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  84.3
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  (3-methyl-2-(morpholin-4-yl)-5-nitrophenyl)methanamine hydrochloride 在 palladium 10% on activated carbon 甲酸铵 、 potassium carbonate 作用下， 以 乙醇 、 乙腈 为溶剂， 反应 48.0h， 生成 3-methyl-4-morpholino-5-(pyrrolidinomethyl)aniline
  参考文献：
  名称：

  [EN] 7-CHLORO-QUINOLIN-4-AMINE COMPOUNDS AND USES THEREOF FOR THE PREVENTION OR TREATMENT OF DISEASES INVOLVING FORMATION OF AMYLOID PLAQUES AND/OR WHERE A DYSFUNCTION OF THE APP METABOLISM OCCURS
  [FR] COMPOSÉS DE 7-CHLORO-QUINOLIN-4-AMINE ET LEURS UTILISATIONS POUR PRÉVENIR OU TRAITER LES MALADIES IMPLIQUANT LA FORMATION DE PLAQUES AMYLOÏDES ET/OU UN DYSFONCTIONNEMENT DU MÉTABOLISME DE L'APP

  摘要：

  本发明涉及具有以下式（I）的化合物，用于预防和/或治疗涉及淀粉样斑块形成和/或APP代谢功能障碍的疾病。

  公开号：

  WO2011073322A1
• 作为产物：
  描述：

  tert-butyl N-([3-methyl-2-(morpholin-4-yl)-5-nitrophenyl]methyl)carbamate 在 甲醇 、 乙酰氯 作用下， 反应 3.0h， 以99%的产率得到(3-methyl-2-(morpholin-4-yl)-5-nitrophenyl)methanamine hydrochloride
  参考文献：
  名称：

  [EN] 7-CHLORO-QUINOLIN-4-AMINE COMPOUNDS AND USES THEREOF FOR THE PREVENTION OR TREATMENT OF DISEASES INVOLVING FORMATION OF AMYLOID PLAQUES AND/OR WHERE A DYSFUNCTION OF THE APP METABOLISM OCCURS
  [FR] COMPOSÉS DE 7-CHLORO-QUINOLIN-4-AMINE ET LEURS UTILISATIONS POUR PRÉVENIR OU TRAITER LES MALADIES IMPLIQUANT LA FORMATION DE PLAQUES AMYLOÏDES ET/OU UN DYSFONCTIONNEMENT DU MÉTABOLISME DE L'APP

  摘要：

  本发明涉及具有以下式（I）的化合物，用于预防和/或治疗涉及淀粉样斑块形成和/或APP代谢功能障碍的疾病。

  公开号：

  WO2011073322A1

文献信息

• NEW HETEROCYCLE COMPOUNDS AND USES THEREOF FOR THE PREVENTION OR TREATMENT OF DISEASES INVOLVING FORMATION OF AMYLOID PLAQUES AND/OR WHERE A DYSFUNCTION OF THE APP METABOLISM OCCURS
  申请人：Delacourte Andre

  公开号：US20120283256A1

  公开（公告）日：2012-11-08

  The present invention relates to compounds having the following Formula (I) for use in the prevention and/or the treatment of diseases involving formation of amyloid plaques and/or where a dysfunction of the APP metabolism occurs.

  本发明涉及具有以下式（I）的化合物，用于预防和/或治疗涉及淀粉样斑块形成和/或APP代谢功能紊乱的疾病。
• Heterocycle compounds and uses thereof for the prevention or treatment of diseases involving formation of amyloid plaques and/or where a dysfunction of the APP metabolism occurs
  申请人：Delacourte Andre

  公开号：US08680095B2

  公开（公告）日：2014-03-25

  The present invention relates to compounds having the following Formula (I) for use in the prevention and/or the treatment of diseases involving formation of amyloid plaques and/or where a dysfunction of the APP metabolism occurs.

  本发明涉及以下式（I）的化合物，用于预防和/或治疗涉及淀粉样斑块形成和/或APP代谢功能障碍的疾病。
• Buchwald reaction as the key step for the synthesis of metabolically more stable analogs of amodiaquine
  作者：Nicolas Le Fur、Guillaume Hochart、Paul-Emmanuel Larchanché、Patricia Melnyk

  DOI：10.1016/j.ejmech.2011.04.047

  日期：2011.7

  Amodiaquine is one of the most active anti-malarial 4-aminoquinoline but its metabolization is believed to generate hepatotoxic derivatives. Previously, we described new analogs of amodiaquine and amopyroquine, in which hydroxyl group was replaced by various amino groups and identified highly potent compounds with lower toxicity. We describe here the synthesis of new analogs that have been modified on their 4'- and 5'-positions in order to reduce their metabolization. A new synthetic strategy was developed using Buchwald coupling reaction as the key step. (C) 2011 Elsevier Masson SAS. All rights reserved.
• 7-CHLORO-QUINOLIN-4-AMINE COMPOUNDS AND USES THEREOF FOR THE PREVENTION OR TREATMENT OF DISEASES INVOLVING FORMATION OF AMYLOID PLAQUES AND/OR WHERE A DYSFUNCTION OF THE APP METABOLISM OCCURS
  申请人：Institut National de la Santé et de la Recherche Médicale

  公开号：EP2513062A1

  公开（公告）日：2012-10-24
• US8680095B2
  申请人：——

  公开号：US8680095B2

  公开（公告）日：2014-03-25