N-[4-(bromomethyl)-6-chloropyridin-2-yl]-N-propylmethanesulfonamide | 853303-83-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: N-[4-(bromomethyl)-6-chloropyridin-2-yl]-N-propylmethanesulfonamide
• CAS: 853303-83-0
• 化学式: C₁₀H₁₄BrClN₂O₂S
• 分子量: 341.656
• InChiKey: PDXXBPUUAZKXGX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  17
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  58.6
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  N-[4-(bromomethyl)-6-chloropyridin-2-yl]-N-propylmethanesulfonamide 、 tert-butyl 1-hydroxy-2-methyl-3-phenylpropan-2-ylcarbamate 在 silver trifluoromethanesulfonate 作用下， 以 二氯甲烷 为溶剂， 反应 19.25h， 生成 tert-butyl [1-benzyl-2-({2-chloro-6-[(methylsulfonyl)(propyl)amino]pyridin-4-yl}methoxy)-1-methylethyl]carbamate
  参考文献：
  名称：

  [EN] BENZYLETHER AND BENZYLAMINO BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
  [FR] INHIBITEURS DE BENZYLETHER ET BENZYLAMINO DE BETA-SECRETASE POUR TRAITER LA MALADIE D'ALZHEIMER

  摘要：

  本发明涉及苯乙醚和苄胺衍生物化合物，这些化合物是β-分泌酶的抑制剂，并且在治疗涉及β-分泌酶的疾病，如阿尔茨海默病中有用。该发明还涉及包含这些化合物的药物组合物，以及在治疗涉及β-分泌酶的这类疾病中使用这些化合物和组合物。

  公开号：

  WO2005051914A1
• 作为产物：
  描述：

  N-[6-chloro-4-(hydroxymethyl)pyridin-2-yl]-N-propylmethanesulfonamide 在 四溴化碳 、 三苯基膦 作用下， 以 二氯甲烷 为溶剂， 反应 0.67h， 生成 N-[4-(bromomethyl)-6-chloropyridin-2-yl]-N-propylmethanesulfonamide
  参考文献：
  名称：

  [EN] BENZYLETHER AND BENZYLAMINO BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
  [FR] INHIBITEURS DE BENZYLETHER ET BENZYLAMINO DE BETA-SECRETASE POUR TRAITER LA MALADIE D'ALZHEIMER

  摘要：

  本发明涉及苯乙醚和苄胺衍生物化合物，这些化合物是β-分泌酶的抑制剂，并且在治疗涉及β-分泌酶的疾病，如阿尔茨海默病中有用。该发明还涉及包含这些化合物的药物组合物，以及在治疗涉及β-分泌酶的这类疾病中使用这些化合物和组合物。

  公开号：

  WO2005051914A1

文献信息

• Benzylether and benzylamino beta-secretase inhibitors for the treatment of alzheimer's disease
  申请人：Nantermet G. Philippe

  公开号：US20070088165A1

  公开（公告）日：2007-04-19

  The present invention is directed to benzylether and benzylamino derivative compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

  本发明涉及式(I)的苯甲醚和苯甲氨基衍生物化合物，它们是β-分泌酶酶的抑制剂，并且在治疗β-分泌酶酶涉及的疾病，例如阿尔茨海默病中有用。本发明还涉及包含这些化合物的制药组合物以及在治疗β-分泌酶酶涉及的疾病中使用这些化合物和组合物的用途。
• Macrocyclic Aminopyridyl Beta-Secretase Inhibitors For The Treatment Of Alzheimer's Disease
  申请人：Nantermet G. Philippe

  公开号：US20080015213A1

  公开（公告）日：2008-01-17

  The present invention is directed to macrocyclic aminopyridyl compounds represented by general formula (I), which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

  本发明涉及由一般式(I)表示的大环氨基吡啶化合物，它们是β-秘酶酶的抑制剂，并且在治疗β-秘酶酶参与的疾病，如阿尔茨海默病中有用。本发明还涉及包含这些化合物的制药组合物以及在治疗β-秘酶酶参与的这些疾病中使用这些化合物和组合物的用途。
• Benzylether and benzylamino beta-secretase inhibitors for the treatment of Alzheimer's disease
  申请人：Merck & Co., Inc.

  公开号：US07354942B2

  公开（公告）日：2008-04-08

  The present invention is directed to benzylether and benzylamino derivative compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

  本发明涉及式（I）的苄醚和苄氨基衍生物化合物，它们是β-分泌酶酶的抑制剂，可用于治疗β-分泌酶酶参与的疾病，如阿尔茨海默病。本发明还涉及包含这些化合物的制药组合物以及使用这些化合物和组合物治疗β-分泌酶酶参与的疾病的方法。
• Macrocyclic aminopyridyl beta-secretase inhibitors for the treatment of Alzheimer's disease
  申请人：Merck, Sharp & Dohme, Corp.

  公开号：US07951949B2

  公开（公告）日：2011-05-31

  The present invention is directed to macrocyclic aminopyridyl compounds represented by general formula (I), which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

  本发明涉及由通式(I)表示的大环氨基吡啶化合物，它们是β-分泌酶酶的抑制剂，并且对于β-分泌酶酶参与的疾病，例如阿尔茨海默病的治疗非常有用。本发明还涉及包含这些化合物的制药组合物以及利用这些化合物和组合物治疗β-分泌酶酶参与的疾病的方法。
• BENZYLETHER AND BENZYLAMINO BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER S DISEASE
  申请人：Merck & Co., Inc.

  公开号：EP1689713A1

  公开（公告）日：2006-08-16