8-fluoro-3,4-dihydro-2(1H)-ketoquinoxaline | 1384067-31-5

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 8-fluoro-3,4-dihydro-2(1H)-ketoquinoxaline
• 英文别名: 8-fluoro-3,4-dihydroquinoxalin-2(1H)-one；8-Fluoro-1,2,3,4-tetrahydroquinoxalin-2-one；8-fluoro-3,4-dihydro-1H-quinoxalin-2-one
• CAS: 1384067-31-5
• 化学式: C₈H₇FN₂O
• mdl: MFCD20544658
• 分子量: 166.155
• InChiKey: PBAXRHGVEHLIDE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.125
• 拓扑面积：
  41.1
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  8-fluoro-3,4-dihydro-2(1H)-ketoquinoxaline 在 sodium hydroxide 、 双氧水 、 三氯氧磷 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 1.75h， 生成 2-氯-8-氟喹喔啉
  参考文献：
  名称：

  Piperazinylquinoxalines with central serotoninmimetic activity

  摘要：

  Regioselective syntheses of substituted 2-chloroquinoxalines and derived 2-(1-piperazinyl)quinoxalines are described. Selectivity in regards to serotonin reuptake blocking and serotoninmimetic activities of the piperazinylquinoxalines is reported. In general, introduction of a 6-substituent into the piperazinylquinoxaline enhanced serotonin reuptake blocking activity and diminished serotoninmimetic activity. Unsubstituted and 3-hydroxypiperazinylquinoxalines had primarily serotoninmimetic activity.

  DOI：

  10.1021/jm00133a019
• 作为产物：
  描述：

  N-(3-fluoro-2-nitrophenyl)glycine ethyl ester 在 盐酸 、 tin 作用下， 以 乙醇 为溶剂， 反应 1.5h， 生成 8-fluoro-3,4-dihydro-2(1H)-ketoquinoxaline
  参考文献：
  名称：

  Piperazinylquinoxalines with central serotoninmimetic activity

  摘要：

  Regioselective syntheses of substituted 2-chloroquinoxalines and derived 2-(1-piperazinyl)quinoxalines are described. Selectivity in regards to serotonin reuptake blocking and serotoninmimetic activities of the piperazinylquinoxalines is reported. In general, introduction of a 6-substituent into the piperazinylquinoxaline enhanced serotonin reuptake blocking activity and diminished serotoninmimetic activity. Unsubstituted and 3-hydroxypiperazinylquinoxalines had primarily serotoninmimetic activity.

  DOI：

  10.1021/jm00133a019

文献信息

• [EN] NON-PEPTIDIC HETEROCYCLE-CONTAINING COMPOUNDS FOR THE TREATMENT OF ALZHEIMER'S DISEASE<br/>[FR] COMPOSÉS NON PÉPTIDIQUES CONTENANT DES HÉTÉROCYCLES POUR LE TRAITEMENT DE LA MALADIE D'ALZHEIMER
  申请人：UNIV ALBERTA

  公开号：WO2020215157A1

  公开（公告）日：2020-10-29

  The present disclosure provides non-peptidic heterocycle-containing amylin receptor antagonist compounds, compositions that include the subject compounds, methods for preparing and using the amylin receptor antagonists, and compositions containing the amylin receptor antagonists for treating, preventing, or ameliorating Alzheimer's disease. Aspects of the present disclosure include a method of inhibiting activity of an amylin receptor by administering to a subject in need thereof a therapeutically effective amount of an amylin receptor antagonist.

  本公开提供了含非肽杂环的胰岛素类受体拮抗剂化合物，包括该类化合物的组合物，用于制备和使用胰岛素类受体拮抗剂的方法，以及含有胰岛素类受体拮抗剂的组合物，用于治疗、预防或改善阿尔茨海默病。本公开的方面包括通过向需要的受试者投与治疗有效量的胰岛素类受体拮抗剂来抑制胰岛素类受体活性的方法。
• Non-Peptidic Heterocycle-Containing Compounds for the Treatment of Alzheimer?s Disease
  申请人：The Governors of the University of Alberta

  公开号：US20220226335A1

  公开（公告）日：2022-07-21

  The present disclosure provides non-peptidic heterocycle-containing amylin receptor antagonist compounds, compositions that include the subject compounds, methods for preparing and using the amylin receptor antagonists, and compositions containing the amylin receptor antagonists for treating, preventing, or ameliorating Alzheimer's disease. Aspects of the present disclosure include a method of inhibiting activity of an amylin receptor by administering to a subject in need thereof a therapeutically effective amount of an amylin receptor antagonist.