3-溴咪唑[1,2-a]吡啶-2-羧酸乙酯 | 143982-54-1

• 物质功能分类: 有机原料 - 杂环化合物
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 中文名称: 3-溴咪唑[1,2-a]吡啶-2-羧酸乙酯
• 中文别名: 3-溴咪唑并[1,2-a]吡啶-2-甲酸乙酯
• 英文名称: Ethyl 3-bromoimidazo[1,2-A]pyridine-2-carboxylate
• CAS: 143982-54-1
• 化学式: C₁₀H₉BrN₂O₂
• mdl: MFCD05864806
• 分子量: 269.09
• InChiKey: MPILHKPXTMEIMG-UHFFFAOYSA-N

物化性质

• 密度：
  1.60±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  43.6
• 氢给体数：
  0
• 氢受体数：
  3

安全信息

• 危险品标志：
  Xi
• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  3-溴咪唑[1,2-a]吡啶-2-羧酸乙酯 、 4,5-双二苯基膦-9,9-二甲基氧杂蒽 、 Dicaesio carbonate 、 水 、 N-甲基吡咯烷酮 在 钯 氮气 、 乙酸乙酯 、 Brine 、 Sodium sulfate-III 、 silica gel 作用下， 反应 10.0h， 以to obtain an amino-imidazo[1,2-a]pyridine-2-carboxylic acid ethyl ester的产率得到3-氨基-2-乙氧基羰基咪唑并[1,2-a]吡啶
  参考文献：
  名称：

  SUBSTITUTED IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS BETA-SECRETASE INHIBITORS

  摘要：

  本发明涉及取代的咪唑并[1,2-a]吡啶衍生物、其药学上可接受的盐以及这些化合物或盐的互变异构体，其抑制β-淀粉样前体蛋白裂解酶（BACE），并且可能在治疗BACE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和使用这些化合物和组合物治疗BACE参与的这些疾病的方法。

  公开号：

  US20120101093A1

文献信息

• [EN] SUBSTITUTED IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS ß-SECRETASE INHIBITORS<br/>[FR] DÉRIVÉS IMIDAZO[1,2-A]PYRIDINE SUBSTITUÉS, COMPOSITIONS PHARMACEUTIQUES, ET PROCÉDÉS D'UTILISATION COMME INHIBITEURS DE LA ?-SÉCRÉTASE
  申请人：HIGH POINT PHARMACEUTICALS LLC

  公开号：WO2010126745A1

  公开（公告）日：2010-11-04

  The present invention is directed to substituted imidazo[1,2-a]pyridine derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE 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 BACE is involved.

  本发明涉及替代咪唑[1,2-a]吡啶衍生物，其药学上可接受的盐，以及这些化合物或盐的互变异构体，其抑制β-淀粉样前体蛋白裂解酶（BACE）并且可能在治疗涉及BACE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BACE的这类疾病中使用这些化合物和组合物。
• [EN] SUBSTITUTED HETEROARYL FUSED DERIVATIVES AS PI3K INHIBITORS<br/>[FR] DÉRIVÉS CONDENSÉS D'HÉTÉROARYLES SUBSTITUÉS À TITRE D'INHIBITEURS DE PI3K
  申请人：INCYTE CORP

  公开号：WO2011075643A1

  公开（公告）日：2011-06-23

  The present invention provides fused derivatives of Formula (I) that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PBKs including, for example, inflammatory disorders, immune- based disorders, cancer, and other diseases.

  本发明提供了公式（I）的融合衍生物，可调节磷脂酰肌醇3-激酶（PI3Ks）的活性，并在治疗与PBKs活性相关的疾病方面具有用处，例如炎症性疾病、免疫性疾病、癌症和其他疾病。
• IMIDAZO[1,2-a]PYRIDINE SULFONAMIDES AS TRPM8 MODULATORS
  申请人：Macielag Mark J.

  公开号：US20120149699A1

  公开（公告）日：2012-06-14

  Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein Y, R 1 , R 2 , and are defined herein.

  揭示了用于治疗各种疾病、综合征、状况和障碍的化合物、组合物和方法，包括疼痛。这些化合物由以下的化学式I代表：其中Y、R1、R2和在此有定义。
• Heteroaryl substituted fused bicyclic heteroaryl compound as GABAA receptor ligands
  申请人：——

  公开号：US20030207885A1

  公开（公告）日：2003-11-06

  This invention relates to heteroaryl substituted fused bicyclic heteroaryl compounds, such as heteroaryl substituted imidazopyridines, imidazopyrazines, imidazopyridizines, imidazopyrimidines, and imidazothiazoles, which may be described by Formula I or Formula II: 1 The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABA A receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Processes for preparing compounds of Formula I and Formula II are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I or Formula II in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABA A receptors in tissue sections.

  本发明涉及杂环取代的融合双环杂环化合物，例如杂环取代的咪唑吡啶、咪唑吡嗪、咪唑吡二嗪、咪唑嘧啶和咪唑噻唑，可以用公式I或公式II描述：1本发明特别涉及与GABAA受体的苯二氮卓位点高选择性和高亲和力结合的这些化合物。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治疗某些中枢神经系统（CNS）疾病的用途。公开了制备公式I和公式II化合物的方法。本发明还涉及使用苯并咪唑、吡啶基咪唑和相关的公式I或公式II的双环杂环化合物与一个或多个其他CNS药物结合，以增强其他CNS药物的作用。此外，本发明还涉及使用这些化合物作为探针来定位组织切片中的GABAA受体。
• Heteroaryl substituted fused bicyclic heteroaryl compounds as GABAA receptor ligands
  申请人：Hutchison Alan

  公开号：US20060014746A1

  公开（公告）日：2006-01-19

  This invention relates to heteroaryl substituted fused bicyclic heteroaryl compounds, such as heteroaryl substituted imidazopyridines, imidazopyrazines, imidazopyridizines, imidazopyrimidines, and imidazothiazoles, which may be described by Formula I or Formula II: The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABA A receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Processes for preparing compounds of Formula I and Formula II are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I or Formula II in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABA A receptors in tissue sections.

  该发明涉及杂环取代融合双环杂环化合物，例如杂环取代咪唑吡啶、咪唑吡嗪、咪唑吡咯、咪唑嘧啶和咪唑噻唑等，可由式I或式II描述：该发明特别涉及与GABAA受体的苯二氮平位点高度选择性和高亲和力结合的这种化合物。该发明还涉及包含这种化合物的药物组合物以及使用这种化合物治疗某些中枢神经系统（CNS）疾病的用途。公开了制备式I和式II化合物的方法。此外，该发明还涉及将苯并咪唑、吡啶基咪唑和相关的式I或式II双环杂环化合物与一个或多个其他CNS药剂联合使用以增强其他CNS药剂的效果。此外，该发明还涉及使用这些化合物作为探针来定位组织切片中的GABAA受体。