AL-34497 | 362512-40-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡唑类
• 英文名称: AL-34497
• 英文别名: 1-(2-aminopropyl)-indazol-6-ol；(2-aminopropyl)-indazol-6-ol；1-(2-aminopropyl)-1H-indazol-6-ol；1-(2-aminopropyl)indazol-6-ol
• CAS: 362512-40-1
• 化学式: C₁₀H₁₃N₃O
• 分子量: 191.233
• InChiKey: WBYHTZYHAFNBKW-UHFFFAOYSA-N

物化性质

• 沸点：
  372.8±22.0 °C(Predicted)
• 密度：
  1.31±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  64.1
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  AL-34497 、 氯甲酸苄酯 在 碳酸氢钠 作用下， 以 四氢呋喃 为溶剂， 生成 [(S)-2-(6-Hydroxy-indazol-1-yl)-l-methylethyl]-carbamic acid benzyl ester
  参考文献：
  名称：

  6-hydroxy-indazole derivatives for treating glaucoma

  摘要：

  披露了用于降低和控制眼压以及治疗青光眼的1-(α-烷基-乙基氨基)-1H-吲哚-6-醇。

  公开号：

  US06956036B1

文献信息

• Pyranoindazoles and their use for the treatment of glaucoma
  申请人：——

  公开号：US20030171418A1

  公开（公告）日：2003-09-11

  Pyranoindazoles are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions containing one or more of the compounds of the present invention.

  吡啶并吡唑类化合物已被披露。还公开了降低和控制正常或升高眼内压力的方法，以及使用含有本发明化合物之一或多个的组合物治疗青光眼的方法。
• PROCESS FOR PREPARING PYRANOINDAZOLE SEROTONERGIC RECEPTOR AGONISTS
  申请人：CONROW Raymond E.

  公开号：US20080033183A1

  公开（公告）日：2008-02-07

  Described are methods of making pyranoindazoles comprising reacting with a reducing agent a protected halohydrin comprising a secondary carbamate to form a pyranoindazole. In preferred embodiments the secondary carbamate is a benzyl carbamate. Also preferred are embodiments wherein the reacting is preceded by reacting a protected halohydrin with a first organometallic compound. The pyranoindazoles thus formed by the described methods are preferably pharmaceutically active products.

  描述了制备吡喃吲唑的方法，包括将含有次级碳酸酯的保护卤代醇与还原剂反应以形成吡喃吲唑。在优选实施例中，次级碳酸酯是苄基碳酸酯。还优选了通过将保护卤代醇与第一有机金属化合物反应来预先进行反应的实施例。因此，通过所述方法形成的吡喃吲唑通常是具有药用活性的产品。
• [EN] METHODS OF MAKING 1-(2-AMINOPROPYL)-6-HYDROXYINDAZOLE<br/>[FR] PROCEDES DE FABRICATION DE 1-(2-AMINOPROPYL)-6-HYDROXYINDAZOLE
  申请人：ALCON INC

  公开号：WO2002098861A1

  公开（公告）日：2002-12-12

  Methods of making 1-(2-aminopropyl)-6-hydroxyindazole are described. The method involves, in part, reacting 4-benzyloxy-2-(2-hydroxypropyl)aminobenzaldehyde with an organic or inorganic nitrite to form 4-benzyloxy-2-(2-hydroxypropyl)nitosaminobenzaldehyde, wich in turn is reacted with a reducing agent with concomitant cyclization to form 6-benzyloxy-1-(2-hydroxypropyl)indazole. The 6-benzyloxy-1-(2-hydroxypropyl)indazole can then be transformed into 1-(2-azidopropyl)-6-benzyloxyindazole which in turn can be converted to the final product.

  描述了制备1-(2-氨丙基)-6-羟基吲唑的方法。该方法包括部分地将4-苄氧基-2-(2-羟基丙基)氨基苯甲醛与有机或无机亚硝酸盐反应，形成4-苄氧基-2-(2-羟基丙基)亚硝胺基苯甲醛，然后与还原剂反应，同时环化形成6-苄氧基-1-(2-羟基丙基)吲唑。然后，6-苄氧基-1-(2-羟基丙基)吲唑可以转化为1-(2-叠氮丙基)-6-苄氧基吲唑，随后可以转化为最终产物。
• Methods of making indazoles
  申请人：——

  公开号：US20040142998A1

  公开（公告）日：2004-07-22

  Methods of making indazoles are described. The methods involved reacting an aromatic aldehyde with a nitrogen source to form a nitroso aromatic aldehyde. The nitroso aromatic aldehyde is reacted with a reducing agent to form an indazole which ultimately can be used to form desired indazoles which are preferably pharmaceutically active products. The process of the present invention further permits the formation of enantiomerically enriched or pure indazoles such as aminoalkyl indazoles.

  本文描述了制备吲唑的方法。该方法涉及将芳香醛与氮源反应以形成亚硝基芳香醛。然后将亚硝基芳香醛与还原剂反应以形成吲唑，最终可以用于形成所需的吲唑，其最好是具有药理活性的产物。本发明的过程进一步允许形成对映富集或纯的吲唑，如氨基烷基吲唑。
• 5-Hydroxy indazole derivatives for treating glaucoma
  申请人：May A. Jesse

  公开号：US20060052431A1

  公开（公告）日：2006-03-09

  3-(2-aminoethyl)-1H-indazol-5-ols useful for treating elevated intraocular pressure and glaucoma are disclosed.

  本发明公开了用于治疗眼压升高和青光眼的3-(2-氨乙基)-1H-吲唑-5-醇。