methyl 1-[(3S)-3-{N,N-dimethylamino}pyrrolidin-1-yl]-2,3-dihydro-1H-indene-5-carboxylate | 1232062-80-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 四氢异喹啉
• 英文名称: methyl 1-[(3S)-3-{N,N-dimethylamino}pyrrolidin-1-yl]-2,3-dihydro-1H-indene-5-carboxylate
• 英文别名: methyl 1-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]-2,3-dihydro-1H-indene-5-carboxylate
• CAS: 1232062-80-4
• 化学式: C₁₇H₂₄N₂O₂
• 分子量: 288.39
• InChiKey: PICZEOMRGBNXCM-LBAUFKAWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.59
• 拓扑面积：
  32.8
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  methyl 1-[(3S)-3-{N,N-dimethylamino}pyrrolidin-1-yl]-2,3-dihydro-1H-indene-5-carboxylate 、 N-(5-氨基-2-甲基苯基)-4-(3-吡啶基)-2-氨基嘧啶 在 三甲基铝 作用下， 以 甲苯 为溶剂， 反应 48.0h， 以60%的产率得到1-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]-N-{4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl}-2,3-dihydro-1H-indene-5-carboxamide
  参考文献：
  名称：

  PREPARATION METHOD OF DIHYDROINDENE AMIDE COMPOUNDS THEIR PHARMACEUTICAL COMPOSITIONS CONTAINING COMPOUNDS THEREOF AND USE AS PROTEIN KINASES INHIBITOR

  摘要：

  公开号：

  EP2385035B1
• 作为产物：
  描述：

  5-溴-1-氯-2,3-二氢-1H-茚 在 1,3-双(二苯基膦)丙烷 、 palladium diacetate potassium carbonate 、 三乙胺 作用下， 以 二甲基亚砜 、 乙腈 为溶剂， 反应 48.0h， 生成 methyl 1-[(3S)-3-{N,N-dimethylamino}pyrrolidin-1-yl]-2,3-dihydro-1H-indene-5-carboxylate
  参考文献：
  名称：

  PREPARATION METHOD OF DIHYDROINDENE AMIDE COMPOUNDS THEIR PHARMACEUTICAL COMPOSITIONS CONTAINING COMPOUNDS THEREOF AND USE AS PROTEIN KINASES INHIBITOR

  摘要：

  公开号：

  EP2385035B1

文献信息

• PREPARATION METHOD OF DIHYDROINDENE AMIDE COMPOUNDS, THEIR PHARMACEUTICAL COMPOSITIONS CONTAINING COMPOUNDS THEREOF AND USE AS PROTEIN KINASES INHIBITOR
  申请人：Yang Xuqing

  公开号：US20110319420A1

  公开（公告）日：2011-12-29

  The invention provides a new kind of dihydroindene amide compounds of general formula I or their pharmaceutically acceptable salts or prodrug thereof which can be used as protein kinase inhibitor. The invention provides a preparation method of the kind of compounds, the pharmaceutical compositions containing the compounds, the method for preventing or curing the diseases related to the abnormity of activities of protein kinases, especially Abl, Bcr-Abl, c-Kit and PDGFR, using them as protein kinase inhibitor, and their preparation use of drug used for preventing or curing the diseases related to the abnormity of activities of protein kinases, especially Abl, Bcr-Abl, c-Kit and PDGFR.

  本发明提供了一种新型的二氢茚酰胺化合物，其通式为I，或其药学上可接受的盐或前药，可用作蛋白激酶抑制剂。本发明还提供了制备该类化合物的方法，含有该化合物的药物组合物，使用它们作为蛋白激酶抑制剂预防或治疗与蛋白激酶活性异常相关的疾病的方法，特别是Abl、Bcr-Abl、c-Kit和PDGFR，以及用于预防或治疗与蛋白激酶活性异常相关的疾病的药物制备用途。
• PREPARATION METHOD OF DIHYDROINDENE AMIDE COMPOUNDS THEIR PHARMACEUTICAL COMPOSITIONS CONTAING COMPOUNDS THEREOF AND USE AS PROTEIN KINASES INHIBITOR
  申请人：Harbin Gloria Pharmaceuticals Co., Ltd.

  公开号：EP2385035A1

  公开（公告）日：2011-11-09

  The invention provides a new kind of dihydroindene amide compounds of general formula I or their pharmaceutically acceptable salts or prodrug thereof which can be used as protein kinase inhibitor. The invention provides a preparation method of the kind of compounds, the pharmaceutical compositions containing the compounds, the method for preventing or curing the diseases related to the abnormity of activities of protein kinases, especially Abl, Bcr-Abl, c-Kit and PDGFR, using them as protein kinase inhibitor, and their preparation use of drug used for preventing or curing the diseases related to the abnormity of activities of protein kinases, especially Abl, Bcr-Abl, c-Kit and PDGFR,

  本发明提供了一种可用作蛋白激酶抑制剂的通式I的新型二氢茚酰胺化合物或其药学上可接受的盐或原药。本发明提供了该类化合物的制备方法、含有该类化合物的药物组合物、将其作为蛋白激酶抑制剂用于预防或治疗与蛋白激酶（尤其是Abl、Bcr-Abl、c-Kit和PDGFR）活性异常有关的疾病的方法，以及将其制备成药物用于预防或治疗与蛋白激酶（尤其是Abl、Bcr-Abl、c-Kit和PDGFR）活性异常有关的疾病的用途、
• US8703771B2
  申请人：——

  公开号：US8703771B2

  公开（公告）日：2014-04-22