ethyl 1-triphenylmethyltetrazol-5-ylacetate | 147284-26-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: ethyl 1-triphenylmethyltetrazol-5-ylacetate
• 英文别名: ethyl (1-trityl-1H-tetrazol-5-yl)acetate；ethyl 2-(1-trityltetrazol-5-yl)acetate
• CAS: 147284-26-2
• 化学式: C₂₄H₂₂N₄O₂
• 分子量: 398.464
• InChiKey: FCKOENQGHBJLBG-UHFFFAOYSA-N

物化性质

• 沸点：
  603.3±55.0 °C(Predicted)
• 密度：
  1.17±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  30
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  69.9
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  ethyl 1-triphenylmethyltetrazol-5-ylacetate 在 sodium hydroxide 、 1-ethyl-3-(3-dimethylamino-propyl)-carbodiimide hydrochloride 作用下， 以 四氢呋喃 、 DMF (N,N-dimethyl-formamide) 、 乙醇 为溶剂， 反应 1.0h， 生成 N-[2-[2-(5-cyano-2-methoxybenzenesulfonylamino)-ethyl]-5-isopropylphenyl]-2-(1-trityl-1H-tetrazol-5-yl)-acetamide
  参考文献：
  名称：

  EP1415983

  摘要：

  公开号：
• 作为产物：
  描述：

  5－甲酸乙酯四氮唑 、 三苯基氯甲烷 在 三乙胺 作用下， 以 四氢呋喃 为溶剂， 反应 2.0h， 生成 ethyl 1-triphenylmethyltetrazol-5-ylacetate
  参考文献：
  名称：

  EP1415983

  摘要：

  公开号：

文献信息

• Heterocyclic amides
  申请人：Zeneca Limited

  公开号：US05521179A1

  公开（公告）日：1996-05-28

  The present invention relates to certain novel heterocyclic amides which are 1-pyridylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic amides, processes for preparing the heterocyclic amides, pharmaceutical compositions containing such heterocyclic amides and methods for their use.

  本发明涉及某些新颖的杂环酰胺，它们是式I所示的1-吡啶乙酰胺化合物，这些化合物是人类白细胞弹性蛋白酶（HLE）的抑制剂，也被称为人类中性粒细胞弹性蛋白酶（HNE），使它们在需要这种抑制作用时非常有用，例如用作药理学、诊断和相关研究工具以及治疗哺乳动物中HLE相关疾病。该发明还包括在合成这些杂环酰胺过程中有用的中间体，制备这些杂环酰胺的方法，含有这些杂环酰胺的药物组合物以及它们的使用方法。
• 5-Amidino-N-(2-aminophenethyl)-2-hydroxybenzenesulfonamide derivative, medicinal composition containing the same, pharmaceutical use thereof, and intermediate therefor
  申请人：Okazaki Kosuke

  公开号：US20060111446A1

  公开（公告）日：2006-05-25

  The present invention relates to a 5-amidino-N-(2-aminophenethyl)-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R 1 is a hydrogen atom or a lower alkyl group; R 2 represents a hydrogen atom, an optionally substituted lower alkyl group, etc.; R 3 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom or a hydroxy group, etc., or a pharmaceutically acceptable salt thereof, which exerts a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.

  本发明涉及一种5-酰胺基-N-(2-氨基苯乙基)-2-羟基苯磺酰胺衍生物，其通式表示为：其中R1为氢原子或低碳基；R2表示氢原子、可选取代的低碳基等；R3为二(低碳基)氨基基团、低碳基、环烷基等；Q为氢原子或可选取代的低碳基；Z为氢原子或羟基等，或其药学上可接受的盐，具有强效和选择性的激活血凝因子X抑制活性，并可用作预防或治疗与激活血凝因子X相关的疾病的药物，以及包含该药物的制药组合物、其药用和中间体。
• 5-amidino-n-(2-aminophenethyl)-n-hydroxy-benzenesulffonamide derivative, medical composition containing the same, pharmaceutical use thereof and intermediate therefor
  申请人：——

  公开号：US20040242455A1

  公开（公告）日：2004-12-02

  The present invention relates to a 5-amidino-N-(2-aminophenethyl)-2-hydroxybenzenesulfonamide derivative represented by the general formula: 1 wherein R 1 is a hydrogen atom or a lower alkyl group; R 2 represents a hydrogen atom, an optionally substituted lower alkyl group, etc.; R 3 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom or a hydroxy group, etc., or a pharmaceutically acceptable salt thereof, which exerts a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.

  本发明涉及一种由通式1表示的5-酰胺基-N-(2-氨基苯乙基)-2-羟基苯磺酰胺衍生物，其中R1是氢原子或较低的烷基；R2表示氢原子、可选取代的较低烷基等；R3是二(较低烷基)氨基基团、较低烷基基团、环烷基等；Q是氢原子或可选取代的较低烷基；Z是氢原子或羟基等，或其药学上可接受的盐，该化合物具有强效和选择性的激活血凝因子X抑制活性，并可用作预防或治疗与激活血凝因子X相关的疾病的药物，以及包含该化合物的制药组合物、其药物用途和中间体。
• Heterocyclic amides having HLE inhibiting activity
  申请人：ZENECA LIMITED

  公开号：EP0509769A2

  公开（公告）日：1992-10-21

  The present invention relates to certain novel heterocyclic amides which are 1-pyridylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic amides, processes for preparing the heterocyclic amides, pharmaceutical compositions containing such heterocyclic amides and methods for their use.

  本发明涉及某些新型杂环酰胺，它们是式I的1-吡啶基乙酰胺化合物，载于本发明中，它们是人白细胞弹性蛋白酶（HLE），也称为人中性粒细胞弹性蛋白酶（HNE）的抑制剂，使得它们在任何需要这种抑制的情况下都有用，例如在药理学、诊断学和相关研究中用作研究工具，以及在治疗哺乳动物中涉及HLE的疾病时。本发明还包括用于合成这些杂环酰胺的中间体、制备杂环酰胺的工艺、含有这些杂环酰胺的药物组合物及其使用方法。
• US5521179A
  申请人：——

  公开号：US5521179A

  公开（公告）日：1996-05-28