7-chloro-8-iodoimidazo[1,2-a]pyridine | 1331823-94-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 英文名称: 7-chloro-8-iodoimidazo[1,2-a]pyridine
• CAS: 1331823-94-9
• 化学式: C₇H₄ClIN₂
• 分子量: 278.48
• InChiKey: VFZAVDXIBMULKG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  11
• 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：
  17.3
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  7-chloro-8-iodoimidazo[1,2-a]pyridine 在 2-双环己基膦-2',6'-二甲氧基联苯 、 potassium dihydrogenphosphate 、 palladium diacetate 作用下， 以 水 、 甲苯 、 乙腈 为溶剂， 反应 5.0h， 生成 tert-butyl 1-(4-(7-phenylimidazo[1,2-a]pyridin-8-yl)phenyl)cyclobutylcarbamate
  参考文献：
  名称：

  Diverse Heterocyclic Scaffolds as Allosteric Inhibitors of AKT

  摘要：

  Wide-ranging exploration of potential replacements for a quinoline-based inhibitor of activation of AKT kinase led to number of alternative, novel scaffolds with potentially improved potency and physicochemical properties. Examples showed predictable DMPK properties, and one such compound demonstrated pharmacodynamic knockdown of phosphorylation of AKT and downstream biomarkers in vivo and inhibition of tumor growth in a breast cancer xenograft model.

  DOI：

  10.1021/jm201394e
• 作为产物：
  描述：

  氯乙醛 、 4-氯-3-碘吡啶-2-胺 以 异丙醇 为溶剂， 以67 %的产率得到7-chloro-8-iodoimidazo[1,2-a]pyridine
  参考文献：
  名称：

  [EN] BCL-XL INHIBITORS
  [FR] INHIBITEURS DE BCL-XL

  摘要：

  Disclosed herein is a compound of Formula (I) for inhibiting Bcl-xL and treating a disease associated with the undesirable Bcl-xL activity (Bcl-xL related diseases), a method of using the compounds disclosed herein for treating tumor or cancer, and a pharmaceutical composition comprising the same.

  公开号：

  WO2023185986A1

文献信息

• [EN] BCL-XL INHIBITORS<br/>[FR] INHIBITEURS DE BCL-XL
  申请人：[en]BEIGENE , LTD.

  公开号：WO2023185986A1

  公开（公告）日：2023-10-05

  Disclosed herein is a compound of Formula (I) for inhibiting Bcl-xL and treating a disease associated with the undesirable Bcl-xL activity (Bcl-xL related diseases), a method of using the compounds disclosed herein for treating tumor or cancer, and a pharmaceutical composition comprising the same.
• Diverse Heterocyclic Scaffolds as Allosteric Inhibitors of AKT
  作者：Jason G. Kettle、Simon Brown、Claire Crafter、Barry R. Davies、Phillippa Dudley、Gary Fairley、Paul Faulder、Shaun Fillery、Hannah Greenwood、Janet Hawkins、Michael James、Keith Johnson、Clare D. Lane、Martin Pass、Jennifer H. Pink、Helen Plant、Sabina C. Cosulich

  DOI：10.1021/jm201394e

  日期：2012.2.9

  Wide-ranging exploration of potential replacements for a quinoline-based inhibitor of activation of AKT kinase led to number of alternative, novel scaffolds with potentially improved potency and physicochemical properties. Examples showed predictable DMPK properties, and one such compound demonstrated pharmacodynamic knockdown of phosphorylation of AKT and downstream biomarkers in vivo and inhibition of tumor growth in a breast cancer xenograft model.