3-溴-6-羟基喹啉 | 13669-57-3

• 物质功能分类: 医药中间体 - 喹啉类化合物
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 中文名称: 3-溴-6-羟基喹啉
• 中文别名: 3 - 溴-6 - 羟基喹啉
• 英文名称: 3-bromoquinolin-6-ol
• 英文别名: 3-bromo-6-hydroxyquinoline
• CAS: 13669-57-3
• 化学式: C₉H₆BrNO
• 分子量: 224.057
• InChiKey: IGCRMJVOMNKTGB-UHFFFAOYSA-N

物化性质

• 沸点：
  348.4±22.0 °C(Predicted)
• 密度：
  1.705±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  33.1
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 海关编码：
  2933499090
• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335

反应信息

• 作为反应物：
  描述：

  3-溴-6-羟基喹啉 在 N-溴代丁二酰亚胺(NBS) 、 偶氮二异丁腈 、 potassium carbonate 、 calcium carbonate 作用下， 以 四氯化碳 、 N,N-二甲基甲酰胺 为溶剂， 反应 7.5h， 生成 (3-bromoquinolin-6-yloxy)methoxy acetic acid methyl ester
  参考文献：
  名称：

  WO2008/110355

  摘要：

  公开号：
• 作为产物：
  描述：

  3-溴喹啉-6-胺 在 磷酸 作用下， 以 乙醇 、 水 为溶剂， 反应 72.0h， 生成 3-溴-6-羟基喹啉
  参考文献：
  名称：

  2,2,3-Tribromopropanal as a Versatile Reagent in the Skraup-Type Synthesis of 3-Bromoquinolin-6-ols

  摘要：

  2,2,3-Tribromopropanal, a reagent which almost became forgotten in the chemical literature after its first application in the 1950s, is used for the one-step transformation of diversely substituted 4-nitro- and 4-methoxyanilines into 3-bromo-6-nitroquinolines and 3-bromo-6-methoxyquinolines. These intermediates are then converted, in one further step, into 3-bromoquinolin-6-ols, which may carry additional substituents at positions 7 and 8.

  DOI：

  10.1055/s-0033-1340670

文献信息

• [EN] SPIRO-FUSED TRICYCLIC MAP4K1 INHIBITORS<br/>[FR] INHIBITEURS DE MAP4K1 TRICYCLIQUES SPIRO FUSIONNÉS
  申请人：BAYER AG

  公开号：WO2021074279A1

  公开（公告）日：2021-04-22

  The present invention relates to Map4K1 inhibitors of formula (I) to pharmaceutical compositions and combinations comprising the compounds according to the invention, and to the prophylactic and therapeutic use of the inventive compounds, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for neoplastic disorders, repectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant MAP4K1 signaling, as a sole agent or in combination with other active ingredients. The present invention further relates to the use, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of protein inhibitors in benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, in neurodegenerative disorders, in inflammatory disorders, in atherosclerotic disorders and in male fertility control.

  本发明涉及式(I)的MAP4K1抑制剂，以及包含根据本发明的化合物的药物组合物和组合物，以及创新化合物的预防性和治疗性用途，分别用于制造用于治疗或预防疾病的药物组合物，特别是用于肿瘤性疾病，癌症或与异常MAP4K1信号相关的其他紊乱免疫反应或其他紊乱的疾病，作为单一药剂或与其他活性成分组合使用。本发明还涉及使用，分别用于制造用于治疗或预防良性增生、动脉粥样硬化疾病、败血症、自身免疫疾病、血管疾病、病毒感染、神经退行性疾病、炎症性疾病、动脉粥样硬化疾病和男性生育控制的蛋白抑制剂的药物组合物的用途。
• [EN] 6 - SUBSTITUTED 3 - (QUINOLIN- 6 - YLTHIO) - [1,2,4] TRIAZOLO [4, 3 -A] PYRADINES AS TYROSINE KINASE<br/>[FR] 3-(QUINOLIN-6-YLTHIO)-[1,2,4]TRIAZOLO[4,3-A]PYRADINES SUBSTITUÉES EN POSITION 6 À ACTIVITÉ TYROSINE KINASE
  申请人：NOVARTIS AG

  公开号：WO2013038362A1

  公开（公告）日：2013-03-21

  The invention relates to compounds of formula (I) and salts thereof: Formula (I) wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).

  该发明涉及公式(I)化合物及其盐：公式(I)其中的取代基如说明书中所定义；用于治疗人体或动物体的公式(I)化合物，特别是针对c-Met酪氨酸激酶介导的疾病或状况；使用公式(I)化合物来制造治疗此类疾病的药物；包含公式(I)化合物的药物组合物，可选地与联合用药伙伴一起使用，以及制备公式(I)化合物的方法。
• [EN] QUINOLIN-, ISOQUINOLIN-, AND QUINAZOLIN-OXYALKYLAMIDES AND THEIR USE AS FUNGICIDES<br/>[FR] OXYALKYLAMIDES DE QUINOLINE, D'ISOQUINOLINE ET DE QUINAZOLINE ET LEUR UTILISATION COMME FONGICIDES
  申请人：SYNGENTA LTD

  公开号：WO2004047538A1

  公开（公告）日：2004-06-10

  Fungicidal compounds of the general formula (1) wherein one of X and Y is N or N-oxide and the other is CR or both of X and Y are N.

  通用公式（1）中的杀真菌化合物，其中X和Y中的一个是N或N-氧化物，另一个是CR，或者X和Y都是N。
• CEREBLON LIGANDS AND BIFUNCTIONAL COMPOUNDS COMPRISING THE SAME
  申请人：Arvinas, Inc.

  公开号：US20180215731A1

  公开（公告）日：2018-08-02

  The description relates to cereblon E3 ligase binding compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present disclosure. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.

  该描述涉及cereblon E3连接酶结合化合物，包括包含相同成分的双功能化合物，这些化合物作为靶向泛素化的调节剂具有实用价值，尤其是抑制剂，可降解和/或以其他方式抑制根据本公开的双功能化合物。特别是，该描述提供了化合物，其一端含有与cereblon E3泛素连接酶结合的配体，另一端含有与目标蛋白结合的部分，使目标蛋白位于泛素连接酶附近以降解（和抑制）该蛋白。可以合成表现出广泛药理活性的化合物，与几乎所有类型的靶向多肽的降解/抑制一致。
• Triazolopyridine Compounds
  申请人：CHEN Chao

  公开号：US20130245002A1

  公开（公告）日：2013-09-19

  The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).

  本发明涉及公式(I)化合物及其盐：其中取代基如说明书中所定义；用于治疗人体或动物体的公式(I)化合物，特别是针对c-Met酪氨酸激酶介导的疾病或状况；使用公式(I)化合物来制造用于治疗这类疾病的药物；包含公式(I)化合物的药物组合物，可选地与联合用药伴侣一起存在，以及制备公式(I)化合物的方法。