tert-butyl (R)-4-(5-aminopyridin-2-yl)-2-methylpiperazine-1-carboxylate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: tert-butyl (R)-4-(5-aminopyridin-2-yl)-2-methylpiperazine-1-carboxylate
• 英文别名: tert-butyl (2R)-4-(5-aminopyridin-2-yl)-2-methylpiperazine-1-carboxylate
• 化学式: C₁₅H₂₄N₄O₂
• 分子量: 292.381
• InChiKey: CIIRBSXWHIXCJU-LLVKDONJSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  71.7
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  tert-butyl (R)-4-(5-aminopyridin-2-yl)-2-methylpiperazine-1-carboxylate 、 2-methylimidazo[1,2-a]pyrazine-6-carboxylic acid 在 N,N-二异丙基乙胺 、 Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以19.5 %的产率得到tert-butyl (R)-2-methyl-4-(5-(2-methylimidazo[1,2-a]pyrazine-6-carboxamido)pyridin-2-yl)piperazine-1-carboxylate
  参考文献：
  名称：

  [EN] HETEROCYCLIC AMIDES AND METHODS OF USING THE SAME
  [FR] AMIDES HÉTÉROCYCLIQUES ET LEURS PROCÉDÉS D'UTILISATION

  摘要：

  The present disclosure relates to compounds of Formula (I), and subformulas thereof, and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds of the present disclosure may act as small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded genes, and methods of use of the compounds for modulating splicing and treating related diseases and conditions. The compounds disclosed herein may possess activity toward various genetic pathways and are accordingly useful in methods of treatment of diseases or disorders of the human or animal body.

  公开号：

  WO2023092098A1
• 作为产物：
  描述：

  tert-butyl (R)-2-methyl-4-(5-nitropyridin-2-yl)piperazine-1-carboxylate 在 palladium 10% on activated carbon 、 氢气 作用下， 以 甲醇 为溶剂， 以99 %的产率得到tert-butyl (R)-4-(5-aminopyridin-2-yl)-2-methylpiperazine-1-carboxylate
  参考文献：
  名称：

  [EN] HETEROCYCLIC AMIDES AND METHODS OF USING THE SAME
  [FR] AMIDES HÉTÉROCYCLIQUES ET LEURS PROCÉDÉS D'UTILISATION

  摘要：

  The present disclosure relates to compounds of Formula (I), and subformulas thereof, and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds of the present disclosure may act as small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded genes, and methods of use of the compounds for modulating splicing and treating related diseases and conditions. The compounds disclosed herein may possess activity toward various genetic pathways and are accordingly useful in methods of treatment of diseases or disorders of the human or animal body.

  公开号：

  WO2023092098A1

文献信息

• PYRIMIDINE COMPOUNDS USEFUL IN THE TREATMENT OF DISEASES MEDIATED BY IKKE AND/OR TBK1 MECHANISMS
  申请人：DOMAINEX LIMITED

  公开号：US20160000784A1

  公开（公告）日：2016-01-07

  Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases IKKε and/or TBK-1 in which one of V and W is N, and the other of V and W is C—H; and R 1 , R 2 , R 3 and R 4 are as defined in the specification. The invention also provides uses of the compounds and compositions containing them.

  通式（I）及其盐在治疗与蛋白激酶IKKε和/或TBK-1的异常活性相关的疾病方面具有用处，其中V和W中的一个是N，另一个是C-H；R1、R2、R3和R4如规范中定义。本发明还提供了化合物的用途和含它们的组合物。
• US9433622B2
  申请人：——

  公开号：US9433622B2

  公开（公告）日：2016-09-06
• [EN] PYRIMIDINE COMPOUNDS USEFUL IN THE TREATMENT OF DISEASES MEDIATED BY IKKE AND/OR TBK1 MECHANISMS<br/>[FR] COMPOSÉS PYRIMIDINE UTILES DANS LE TRAITEMENT DE MALADIES MÉDIÉES PAR LES MÉCANISMES DES IKK&Egr; ET/OU TBK-1
  申请人：DOMAINEX LTD

  公开号：WO2014128486A1

  公开（公告）日：2014-08-28

  Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases ΙΚΚε and/or TBK-1 in which one of V and W is N, and the other of V and W is C-H; and R1, R2, R3 and R4 are as defined in the specification. The invention also provides uses of the compounds and compositions containing them.