6-(3,3-diethoxyprop-1-yn-1-yl)quinoline | 1197377-23-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 6-(3,3-diethoxyprop-1-yn-1-yl)quinoline
• 英文别名: 6-(3,3-diethoxyprop-1-ynyl)quinoline
• CAS: 1197377-23-3
• 化学式: C₁₆H₁₇NO₂
• 分子量: 255.316
• InChiKey: LCQXEYSBXHETDM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  19
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  31.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  6-(3,3-diethoxyprop-1-yn-1-yl)quinoline 在 钯 氢气 、 四氢呋喃 作用下， 以 四氢呋喃 为溶剂， 反应 6.0h， 以to afford 6-(3,3-diethoxypropyl)quinoline (23, 56 mg, 57 mg theoretical, 98% yield) as a clear oil, which的产率得到6-(3,3-diethoxypropyl)quinoline
  参考文献：
  名称：

  Salts of 2-fluoro-N-methyl-4-[7-(quinolin-6-yl-methyl)-imidazo[1,2-B][1,2,4]triazin-2-yl]benzamide and processes related to preparing the same

  摘要：

  本发明涉及二氢氯酸和二苯磺酸盐的c-Met激酶抑制剂2-氟-N-甲基-4-[7-(喹啉-6-基甲基)-咪唑[1,2-b][1,2,4]三嗪-2-基]苯甲酰胺及其制药组合物，用于治疗癌症和其他与激酶通路失调相关的疾病。本发明还涉及制备2-氟-N-甲基-4-[7-(喹啉-6-基甲基)咪唑[1,2-b][1,2,4]三嗪-2-基]苯甲酰胺及其盐的过程和中间体。

  公开号：

  US08901123B2
• 作为产物：
  描述：

  6-溴喹啉 、 丙醛二乙基乙缩醛 在 potassium phosphate 、 N-(2,6-dimethylphenyl)-N’-(pyridin-2-ylmethyl)oxalamide 、 copper(l) chloride 作用下， 以 叔丁醇 为溶剂， 以80%的产率得到6-(3,3-diethoxyprop-1-yn-1-yl)quinoline
  参考文献：
  名称：

  Cu/草酸二酰胺催化末端炔烃与芳基卤化物的偶联

  摘要：

  N 1 -(2,6-二甲基苯基)- N 2 -(吡啶-2-基甲基)草酰胺 (DMPPO) 被发现是铜催化的（杂）芳基卤化物与 1-炔烃偶联反应的更有效配体以前报道过的。仅需 3 mol% CuCl 和 DMPPO 即可在 100 °C（溴化物）和 80 °C（碘化物）下完成偶联。（杂）芳基和烷基取代的 1-炔烃在这些条件下都表现良好，导致内部炔烃的形成具有很大的多样性。

  DOI：

  10.1021/acs.joc.2c02882

文献信息

• SALTS OF 2-FLUORO-N-METHYL-4-[7-(QUINOLIN-6-YL-METHYL)-IMIDAZO[1,2-b][1,2,4]TRIAZIN-2-YL]BENZAMIDE AND PROCESSES RELATED TO PREPARING THE SAME
  申请人：Weng Lingkai

  公开号：US20090291956A1

  公开（公告）日：2009-11-26

  The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.

  本发明涉及二氢氯酸和二苯磺酸盐的c-Met激酶抑制剂2-氟-N-甲基-4-[7-(喹啉-6-基甲基)-咪唑[1,2-b][1,2,4]三嗪-2-基]苯甲酰胺，以及其制药组合物，在癌症和其他与激酶途径失调相关的疾病治疗中有用。本发明还涉及用于制备2-氟-N-甲基-4-[7-(喹啉-6-基甲基)咪唑[1,2-b][1,2,4]三嗪-2-基]苯甲酰胺及其盐的工艺和中间体。
• SALTS OF 2-FLUORO-N-METHYL-4-[7-(QUINOLIN-6-YL-METHYL)-IMIDAZO[1,2-B][1,2,4]TRIAZIN-2-YL]BENZAMIDE AND PROCESSES RELATED TO PREPARING THE SAME
  申请人：WENG Lingkai

  公开号：US20130289036A1

  公开（公告）日：2013-10-31

  The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.

  本发明涉及c-Met激酶抑制剂2-氟-N-甲基-4-[7-(喹啉-6-基甲基)-咪唑[1,2-b][1,2,4]三嗪-2-基]苯甲酰胺的二盐酸盐和二苯磺酸盐，以及其制备的医药组合物，可用于治疗癌症和与激酶途径失调相关的其他疾病。本发明还涉及制备2-氟-N-甲基-4-[7-(喹啉-6-基甲基)咪唑[1,2-b][1,2,4]三嗪-2-基]苯甲酰胺及其盐的过程和中间体。
• Salts of 2-fluoro-N-methyl-4-[7-(quinolin-6-yl-methyl)-imidazo[1,2-B][1,2,4]triazin-2-yl]benzamide and processes related to preparing the same
  申请人：Weng Lingkai

  公开号：US08901123B2

  公开（公告）日：2014-12-02

  The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.

  本发明涉及二氢氯酸和二苯磺酸盐的c-Met激酶抑制剂2-氟-N-甲基-4-[7-(喹啉-6-基甲基)-咪唑[1,2-b][1,2,4]三嗪-2-基]苯甲酰胺及其制药组合物，用于治疗癌症和其他与激酶通路失调相关的疾病。本发明还涉及制备2-氟-N-甲基-4-[7-(喹啉-6-基甲基)咪唑[1,2-b][1,2,4]三嗪-2-基]苯甲酰胺及其盐的过程和中间体。
• Salts of 2-fluoro-N-methyl-4-[7-(quinolin-6-yl-methyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide and processes related to preparing the same
  申请人：Weng Lingkai

  公开号：US08420645B2

  公开（公告）日：2013-04-16

  The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.

  本发明涉及c-Met激酶抑制剂2-氟-N-甲基-4-[7-(喹啉-6-基甲基)-咪唑[1,2-b][1,2,4]三嗪-2-基]苯甲酰胺的双盐酸和二苯磺酸盐，以及其制备的药物组合物，用于治疗癌症和与激酶通路失调相关的其他疾病。本发明还涉及制备2-氟-N-甲基-4-[7-(喹啉-6-基甲基)咪唑[1,2-b][1,2,4]三嗪-2-基]苯甲酰胺及其盐的过程和中间体。
• SALTS OF 2-FLUORO-N-METHYL-4-[7-(QUINOLIN-6-YL-METHYL) - IMIDAZO [1, 2-B] [1, 2, 4] TRIAZIN-2-YL] BENZAMIDE AND PROCESSES RELATED TO PREPARING THE SAME
  申请人：Incyte Corporation

  公开号：EP2300455A2

  公开（公告）日：2011-03-30