1,2-di(4-N,N-dimethylamino-phenyl)-1H-imidazo[4,5-b]pyrazine | 1350629-12-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 1,2-di(4-N,N-dimethylamino-phenyl)-1H-imidazo[4,5-b]pyrazine
• 英文别名: 4-[3-[4-(dimethylamino)phenyl]imidazo[4,5-b]pyrazin-2-yl]-N,N-dimethylaniline
• CAS: 1350629-12-7
• 化学式: C₂₁H₂₂N₆
• 分子量: 358.446
• InChiKey: NXWJPKNBSJCENU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  50.1
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  2,3-二氯吡嗪 、 4-(dimethylamino)-N-(4-(dimethylamino)phenyl)benzimidamide 在 palladium diacetate 、 4,5-双二苯基膦-9,9-二甲基氧杂蒽 、 sodium t-butanolate 作用下， 以 甲苯 为溶剂， 反应 24.0h， 以79%的产率得到1,2-di(4-N,N-dimethylamino-phenyl)-1H-imidazo[4,5-b]pyrazine
  参考文献：
  名称：

  可调荧光发射的1,2-二取代（杂）芳基稠合咪唑的区域专一性合成

  摘要：

  建立了钯催化的两倍或四倍胺化反应，该反应可以区域特异性合成1,2-二取代（杂）芳基稠合的咪唑的多样性导向文库，并为发现具有可调荧光发射的荧光支架提供了出色的工具。这些荧光团已被用作活细胞成像的荧光探针。

  DOI：

  10.1021/ol202807d

文献信息

• COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH APJ RECEPTOR ACTIVITY
  申请人：Annapurna Bio, Inc.

  公开号：US20220125787A1

  公开（公告）日：2022-04-28

  This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize) the apelin receptor (also referred to herein as the APJ receptor; gene symbol APLNR). This disclosure also features compositions containing the same as well as other methods of using and making the same. The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which a decrease in APJ receptor activity (e.g., repressed or impaired APJ receptor signaling; e.g., repressed or impaired apelin-APJ receptor signaling) or downregulation of endogenous apelin contributes to the pathology and/or symptoms and/or progression of the disease, disorder, or condition. Non-limiting examples of such diseases, disorders, or conditions include: (i) cardiovascular disease; (ii) metabolic disorders; (iii) diseases, disorders, and conditions associated with vascular pathology; and (iv) organ failure; (v) diseases, disorders, and conditions associated with infections (e.g., microbial infections); and (vi) diseases, disorders, or conditions that are sequela or comorbid with any of the foregoing or any disclosed herein. More particular non-limiting examples of such diseases, disorders, or conditions include pulmonary hypertension (e.g., PAH); heart failure; type II diabetes; renal failure; sepsis; and systemic hypertension.
• [EN] COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH APJ RECEPTOR ACTIVITY<br/>[FR] COMPOSÉS ET COMPOSITIONS DESTINÉS AU TRAITEMENT D'ÉTATS PATHOLOGIQUES ASSOCIÉS À UNE ACTIVITÉ DU RÉCEPTEUR DE L'APJ
  申请人：ANNAPURNA BIO INC

  公开号：WO2020073011A1

  公开（公告）日：2020-04-09

  This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize) the apelin receptor (also referred to herein as the APJ receptor; gene symbol APLNR). This disclosure also features compositions containing the same as well as other methods of using and making the same. The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which a decrease in APJ receptor activity (e.g., repressed or impaired APJ receptor signaling; e.g., repressed or impaired apelin-APJ receptor signaling) or downregulation of endogenous apelin contributes to the pathology and/or symptoms and/or progression of the disease, disorder, or condition. Non-limiting examples of such diseases, disorders, or conditions include: (i) cardiovascular disease; (ii) metabolic disorders; (iii) diseases, disorders, and conditions associated with vascular pathology; and (iv) organ failure; (v) diseases, disorders, and conditions associated with infections (e.g., microbial infections); and (vi) diseases, disorders, or conditions that are sequela or comorbid with any of the foregoing or any disclosed herein. More particular non-limiting examples of such diseases, disorders, or conditions include pulmonary hypertension (e.g., PAH); heart failure; type II diabetes; renal failure; sepsis; and systemic hypertension.