2,3-二氯-5-(三氟甲基)吡嗪 | 1238230-17-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 中文名称: 2,3-二氯-5-(三氟甲基)吡嗪
• 英文名称: 2,3-dichloro-5-(trifluoromethyl)pyrazine
• CAS: 1238230-17-5
• 化学式: C₅HCl₂F₃N₂
• 分子量: 216.978
• InChiKey: QISCHXLTPQIMCO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  25.8
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2,3-二氯-5-(三氟甲基)吡嗪 在 盐酸 、 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 tris-(dibenzylideneacetone)dipalladium(0) 、 sodium cyanoborohydride 、 sodium carbonate 、 caesium carbonate 、 R-(+)-1,1'-联萘-2,2'-双二苯膦 作用下， 以 1,4-二氧六环 、 甲醇 、 甲苯 为溶剂， 20.0~110.0 ℃ 、101.33 kPa 条件下， 反应 51.0h， 生成
  参考文献：
  名称：

  [EN] N-(HETEROCYCLYL AND HETEROCYCLYLALKYL)-3-BENZYLPYRIDIN-2-AMINE DERIVATIVES AS SSTR4 AGONISTS
  [FR] DÉRIVÉS DE N-(HÉTÉROCYCLYL ET HÉTÉROCYCLYLALKYL)-3-BENZYLPYRIDIN-2-AMINE SERVANT D'AGONISTES DE SSTR4

  摘要：

  披露了公式（1）的化合物，以及其中n、R1、R4、R5、R6、R7、R8、R9、R10、R11、R14、X2、X3和X12在说明书中定义的药用可接受盐。本公开还涉及用于制备公式（1）化合物的材料和方法，含有它们的药物组合物，以及它们用于治疗与SSTR4相关的疾病、障碍和状况。

  公开号：

  WO2021202775A1

文献信息

• Herstellung von halogenierten N-heteroaromatischen Polyhalogenderivaten
  申请人：Saltigo GmbH

  公开号：EP2213663A1

  公开（公告）日：2010-08-04

  Die vorliegende Erfindung betrifft ein Verfahren zur Herstellung von halogenierten N-heteroaromatischen Polyhalogenderivaten.

  本发明涉及一种卤代 N-杂芳香族多卤素衍生物的制备工艺。
• AMINOPYRAZINES AND RELATED COMPOUNDS USEFUL AS MITOCHONDRIAL UNCOUPLERS
  申请人：VIRGINIA TECH INTELLECTUAL PROPERTIES, INC.

  公开号：US20210253538A1

  公开（公告）日：2021-08-19

  The disclosure provides compounds of Formula I and the pharmaceutically acceptable salts thereof. The variables, R 1 , R 2 , R 3 , R 4 , R 5 , X 1 , X 2 , and Z are defined herein. Certain compounds of Formula I act as selective mitochondrial protonophore uncouplers that do not affect the plasma membrane potential. The disclosure includes pharmaceutical composition comprising a compound or salt Formula I, and a pharmaceutically acceptable carrier. Compounds and salts of Formula I are useful for treating or decreasing the risk of conditions responsive to mitochondrial uncoupling, such as obesity, cancer, type II diabetes, fatty liver disease, insulin resistance, Parkinson's disease, ischemia reperfusion injury, heart failure, non-alcoholic fatty liver disease (NALFD), and non-alcoholic steatohepatitis (NASH). Because mitochondrial uncouplers decrease the production of reactive oxygen species (ROS), which are known to contribute to age-related cell damage, compounds of Formula I are useful for increasing lifespan. Compounds and salts of Formula I are also useful for regulating glucose homeostasis or insulin action in a patient.
• [EN] AMINOPYRAZINES AND RELATED COMPOUNDS USEFUL AS MITOCHONDRIAL UNCOUPLERS<br/>[FR] AMINOPYRAZINES ET COMPOSÉS APPARENTÉS UTILISABLES EN TANT QUE DÉCOUPLEURS MITOCHONDRIAUX
  申请人：VIRGINIA TECH INTELLECTUAL PROPERTIES INC

  公开号：WO2019204819A1

  公开（公告）日：2019-10-24

  The disclosure provides compounds of Formula I and the pharmaceutically acceptable salts thereof. The variables, R1, R2, R3, R4, R5, X1, X2, and Z are defined herein. Certain compounds of Formula I act as selective mitochondrial protonophore uncouplers that do not affect the plasma membrane potential. The disclosure includes pharmaceutical composition comprising a compound or salt Formula I, and a pharmaceutically acceptable carrier. Compounds and salts of Formula I are useful for treating or decreasing the risk of conditions responsive to mitochondrial uncoupling, such as obesity, cancer, type II diabetes, fatty liver disease, insulin resistance, Parkinson's disease, ischemia reperfusion injury, heart failure, non-alcoholic fatty liver disease (NALFD), and non-alcoholic steatohepatitis (NASH). Because mitochondrial uncouplers decrease the production of reactive oxygen species (ROS), which are known to contribute to age-related cell damage, compounds of Formula I are useful for increasing lifespan. Compounds and salts of Formula I are also useful for regulating glucose homeostasis or insulin action in a patient.
• [EN] N-(HETEROCYCLYL AND HETEROCYCLYLALKYL)-3-BENZYLPYRIDIN-2-AMINE DERIVATIVES AS SSTR4 AGONISTS<br/>[FR] DÉRIVÉS DE N-(HÉTÉROCYCLYL ET HÉTÉROCYCLYLALKYL)-3-BENZYLPYRIDIN-2-AMINE SERVANT D'AGONISTES DE SSTR4
  申请人：TAKEDA PHARMACEUTICALS CO

  公开号：WO2021202775A1

  公开（公告）日：2021-10-07

  Disclosed are compounds of Formula (1), and pharmaceutically acceptable salts thereof, wherein n, R1, R4, R5, R6, R7, R8, R9, R10, R11, R14, X2, X3 and X12 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula (1), to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with SSTR4.

  披露了公式（1）的化合物，以及其中n、R1、R4、R5、R6、R7、R8、R9、R10、R11、R14、X2、X3和X12在说明书中定义的药用可接受盐。本公开还涉及用于制备公式（1）化合物的材料和方法，含有它们的药物组合物，以及它们用于治疗与SSTR4相关的疾病、障碍和状况。