6-bromo-N-isopropylquinazolin-4-amine | 307538-41-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 6-bromo-N-isopropylquinazolin-4-amine
• 英文别名: 6-bromo-4-isopropylaminoquinazoline；6-bromo-N-(propan-2-yl)quinazolin-4-amine；6-bromo-N-propan-2-ylquinazolin-4-amine
• CAS: 307538-41-6
• 化学式: C₁₁H₁₂BrN₃
• 分子量: 266.14
• InChiKey: CZZPGAMGPKBBPA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  37.8
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  6-bromo-N-isopropylquinazolin-4-amine 、 三丁基噻唑-5-锡 在 copper(l) iodide 、 1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物 、 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 0.08h， 生成 N-isopropyl-6-(thiazol-5-yl)quinazolin-4-amine
  参考文献：
  名称：

  Discovery, Synthesis, and Biological Evaluation of Thiazoloquin(az)olin(on)es as Potent CD38 Inhibitors

  摘要：

  A series of thiazoloquin(az)olinones were synthesized and found to have potent inhibitory activity against CD38. Several of these compounds were also shown to have good pharmacokinetic properties and demonstrated the ability to elevate NAD levels in plasma, liver, and muscle tissue. In particular, compound 78c was given to diet induced obese (DIO) C57Bl6 mice, elevating NAD > 5-fold in liver and >1.2-fold in muscle versus control animals at a 2 h time point. The compounds described herein possess the most potent CD38 inhibitory activity of any small molecules described in the literature to date. The inhibitors should allow for a more detailed assessment of how NAD elevation via CD38 inhibition affects physiology in NAD deficient states.

  DOI：

  10.1021/jm502009h
• 作为产物：
  描述：

  6-溴-4-氯喹唑啉 、 异丙胺 以 乙腈 为溶剂， 生成 6-bromo-N-isopropylquinazolin-4-amine
  参考文献：
  名称：

  Discovery, Synthesis, and Biological Evaluation of Thiazoloquin(az)olin(on)es as Potent CD38 Inhibitors

  摘要：

  A series of thiazoloquin(az)olinones were synthesized and found to have potent inhibitory activity against CD38. Several of these compounds were also shown to have good pharmacokinetic properties and demonstrated the ability to elevate NAD levels in plasma, liver, and muscle tissue. In particular, compound 78c was given to diet induced obese (DIO) C57Bl6 mice, elevating NAD > 5-fold in liver and >1.2-fold in muscle versus control animals at a 2 h time point. The compounds described herein possess the most potent CD38 inhibitory activity of any small molecules described in the literature to date. The inhibitors should allow for a more detailed assessment of how NAD elevation via CD38 inhibition affects physiology in NAD deficient states.

  DOI：

  10.1021/jm502009h

文献信息

• Substituted 4-Amino-Quinazoline Compounds with Metabotropic Glutamate Receptor Regulating Activity and Uses Thereof
  申请人：REICH Melanie

  公开号：US20090069320A1

  公开（公告）日：2009-03-12

  Substituted 4-amino-quinazoline compounds corresponding to formula I methods for their production, pharmaceutical compositions containing these compounds as active agents, and the uses thereof for treating or inhibiting disorders or disease states.

  根据公式I的4-氨基喹唑啉化合物替代物，其生产方法，含有这些化合物的药物组合物以及用于治疗或抑制疾病状态或疾病状态的用途。
• NOVEL SULPHOXIMINE-SUBSTITUTED QUINOLINE AND QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS
  申请人：EIS Knut

  公开号：US20090226377A1

  公开（公告）日：2009-09-10

  The present invention relates to a quinoline or quinazoline derivative having the general formula (A): in which R 3 , R 4 , W, Y and Q are indicated in the description and the claims, the use of the compounds of the general formula (A) for the treatment of various disorders, and the preparation of compounds of the general formula (A).

  本发明涉及一种具有通式（A）的喹啉或喹嗪衍生物，其中R3、R4、W、Y和Q在说明书和权利要求书中指示，通式（A）化合物用于治疗各种疾病，以及通式（A）化合物的制备。
• WO2008/141843
  申请人：——

  公开号：——

  公开（公告）日：——
• NOVEL SULPHOXIMINE-SUBSTITUTED QUINAZOLINE AND QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS
  申请人：Bayer Schering Pharma Aktiengesellschaft

  公开号：EP2152672A1

  公开（公告）日：2010-02-17
• Identification of CDKI pathway inhibitors
  申请人：Chang Bey-Dih

  公开号：US20080033000A1

  公开（公告）日：2008-02-07

  The invention relates to the inhibition of the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. More particularly, the invention relates to methods for inhibiting the CDKI pathway for studies of and intervention in senescence-related and other CDKI-related diseases.