5,7-dibromo-2-methylquinoline | 1312180-15-6

• 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
• 英文名称: 5,7-dibromo-2-methylquinoline
• 英文别名: 5,7-Dibromo-2-methylquinoline
• CAS: 1312180-15-6
• 化学式: C₁₀H₇Br₂N
• 分子量: 300.98
• InChiKey: CMZZDUIVBSRZHM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  12.9
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  5,7-dibromo-2-methylquinoline 、 4-氟苯硼酸 在 palladium diacetate 、 caesium carbonate 作用下， 以 N-甲基吡咯烷酮 、 水 为溶剂， 反应 12.0h， 生成
  参考文献：
  名称：

  Studies of one-pot double couplings on dibromoquinolines

  摘要：

  In a series of studies, the regioselectivity of Suzuki couplings of dibromoquinolines has been investigated. In general, it is much harder to achieve high levels of regioselectivity in these systems compared to many of the other dibromoheteroaromatics that have been studied. Useful levels of selectivity could be achieved for both a 5,7-dibromoquinoline as well as 3,4-dibromoquinoline. Double Suzuki couplings could also be achieved on these two compounds. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2011.04.052
• 作为产物：
  描述：

  2,6-二溴-4-硝基苯胺 在 盐酸 、 硫酸 、 sodium nitrite 作用下， 以 乙醇 、 水 为溶剂， 生成 5,7-dibromo-2-methylquinoline
  参考文献：
  名称：

  Studies of one-pot double couplings on dibromoquinolines

  摘要：

  In a series of studies, the regioselectivity of Suzuki couplings of dibromoquinolines has been investigated. In general, it is much harder to achieve high levels of regioselectivity in these systems compared to many of the other dibromoheteroaromatics that have been studied. Useful levels of selectivity could be achieved for both a 5,7-dibromoquinoline as well as 3,4-dibromoquinoline. Double Suzuki couplings could also be achieved on these two compounds. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2011.04.052

文献信息

• FUSED RING COMPOUND AND APPLICATION THEREOF
  申请人：Wuhan LL Science and Technology Development Co., Ltd.

  公开号：EP4079724A1

  公开（公告）日：2022-10-26

  Disclosed is a fused ring compound and an application thereof. Disclosed is a fused ring compound represented by formula I, a pharmaceutically acceptable salt, a stereoisomer, a tautomer, an isotope compound, a crystal form, a nitrogen oxide, a solvate, or a solvate of the pharmaceutically acceptable salt thereof. The fused ring compound of the present invention has high P2X4 antagonistic activity, excellent selectivity, low toxicity and excellent metabolic stability.

  本发明公开了一种融合环化合物及其应用。公开了一种由公式I表示的融合环化合物，其药学上可接受的盐、立体异构体、互变异构体、同位素化合物、晶体形态、氮氧化物、溶剂合物或其药学上可接受的盐的溶剂合物。本发明的融合环化合物具有高P2X4拮抗活性、优异的选择性、低毒性和优异的代谢稳定性。
• Tetrahydroquinoline derivatives and their use as Epac inhibitors
  申请人：Institut National de la Sante et de la Recherche Medicale (INSERM)

  公开号：US10093627B2

  公开（公告）日：2018-10-09

  The invention relates to tetrahydroquinoline derivatives and their use in the treatment and/or the prevention of a disease wherein the Epac protein is involved, such as inflammation, cancer, vascular diseases, kidney diseases, cognitive disorders and cardiac diseases.

  本发明涉及四氢喹啉衍生物及其在治疗和/或预防涉及 Epac 蛋白的疾病（如炎症、癌症、血管疾病、肾脏疾病、认知障碍和心脏病）中的用途。
• TETRAHYDROQUINOLINE DERIVATIVES AND THEIR USE AS EPAC INHIBITORS
  申请人：Institut National de la Santé et de la Recherche Médicale (INSERM)

  公开号：EP2903612A1

  公开（公告）日：2015-08-12
• Tetrahydroquinoline Derivatives and Their Use as Epac Inhibitors
  申请人：Institut National de la Sante et de la Recherche Medicale (INSERM)

  公开号：US20180009757A1

  公开（公告）日：2018-01-11

  The invention relates to tetrahydroquinoline derivatives and their use in the treatment and/or the prevention of a disease wherein the Epac protein is involved, such as inflammation, cancer, vascular diseases, kidney diseases, cognitive disorders and cardiac diseases.
• US9751838B2
  申请人：——

  公开号：US9751838B2

  公开（公告）日：2017-09-05