t-butyl 4-(methylamino)isoindoline-2-carboxylate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: t-butyl 4-(methylamino)isoindoline-2-carboxylate
• 英文别名: Tert-butyl 4-(methylamino)-1,3-dihydroisoindole-2-carboxylate；tert-butyl 4-(methylamino)-1,3-dihydroisoindole-2-carboxylate
• 化学式: C₁₄H₂₀N₂O₂
• 分子量: 248.325
• InChiKey: OEPCAPWLSOZZFC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  41.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  t-butyl 4-(methylamino)isoindoline-2-carboxylate 在 盐酸 作用下， 以 1,4-二氧六环 为溶剂， 以100 %的产率得到N-methylisoindolin-4-amine hydrochloride
  参考文献：
  名称：

  [EN] ISOINDOLINES AS PMS2 INHIBITORS
  [FR] ISOINDOLINES EN TANT QU'INHIBITEURS DE PMS2

  摘要：

  The present invention relates to compounds of Formula (II) that target the PMS2 proteins that are components of the DNA Mismatch Repair (MMR) process wherein R2, R4, R6, Y1, Y2, A1, A2, A3, and A4are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PMS2 activity is implicated.

  公开号：

  WO2023094834A1
• 作为产物：
  描述：

  4-溴异吲哚啉-2-羧酸叔丁酯 、 盐酸甲胺 在 tris-(dibenzylideneacetone)dipalladium(0) 、 2-(二环己基膦)3,6-二甲氧基-2′,4′,6′-三异丙基-1,1′-联苯 、 sodium t-butanolate 作用下， 以 1,4-二氧六环 为溶剂， 以18 %的产率得到t-butyl 4-(methylamino)isoindoline-2-carboxylate
  参考文献：
  名称：

  [EN] ISOINDOLINES AS PMS2 INHIBITORS
  [FR] ISOINDOLINES EN TANT QU'INHIBITEURS DE PMS2

  摘要：

  The present invention relates to compounds of Formula (II) that target the PMS2 proteins that are components of the DNA Mismatch Repair (MMR) process wherein R2, R4, R6, Y1, Y2, A1, A2, A3, and A4are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PMS2 activity is implicated.

  公开号：

  WO2023094834A1

文献信息

• Macrocyclic Heterocyclic Compound for Inhibiting Hepatitis C Virus and Preparation and Use Thereof
  申请人：Zhan Zheng-yun James

  公开号：US20140205567A1

  公开（公告）日：2014-07-24

  The present invention discloses a class of novel macro-heterocyclic compounds represented by the formula Ia or Ib, and their intermediates, preparation methods and the uses. The macro-heterocyclic compounds of the present invention have good inhibitory activities against hepatitis C virus (HCV), and can be used to treat HCV infection effectively by its excellent inhibition against HCV, low toxicity and side effects.

  本发明公开了一类新型大环杂环化合物，其代表性结构式为Ia或Ib，及其中间体、制备方法和用途。本发明的大环杂环化合物对丙型肝炎病毒（HCV）具有良好的抑制活性，凭借其对HCV的优异抑制作用、低毒性和副作用，能有效用于治疗HCV感染。
• US8962810B2
  申请人：——

  公开号：US8962810B2

  公开（公告）日：2015-02-24
• [EN] ISOINDOLINES AS PMS2 INHIBITORS<br/>[FR] ISOINDOLINES EN TANT QU'INHIBITEURS DE PMS2
  申请人：[en]NEOPHORE LIMITED

  公开号：WO2023094834A1

  公开（公告）日：2023-06-01

  The present invention relates to compounds of Formula (II) that target the PMS2 proteins that are components of the DNA Mismatch Repair (MMR) process wherein R2, R4, R6, Y1, Y2, A1, A2, A3, and A4are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PMS2 activity is implicated.