4-((5-bromothiophen-3-yl)methyl)morpholine | 364794-05-8

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 4-((5-bromothiophen-3-yl)methyl)morpholine
• 英文别名: 4-[(5-Bromothiophen-3-yl)methyl]morpholine
• CAS: 364794-05-8
• 化学式: C₉H₁₂BrNOS
• 分子量: 262.17
• InChiKey: CORIIGSQWGBPIR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  40.7
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  7-bromo-4-[(2,4-dichloro-5-methoxyphenyl)amino]-3-quinolinecarbonitrile 、 4-((5-bromothiophen-3-yl)methyl)morpholine 在 四(三苯基膦)钯 、 碳酸氢钠 作用下， 以 乙二醇二甲醚 为溶剂， 生成 4-(2,4-dichloro-5-methoxyanilino)-7-[4-(4-morpholinylmethyl)-thien-2-yl]-3-quinolinecarbonitrile
  参考文献：
  名称：

  Inhibition of Src kinase activity by 4-anilino-7-thienyl-3-quinolinecarbonitriles

  摘要：

  Based on a screening lead from a yeast-based assay to identify Src family kinase inhibitors, a series of 4-anilino-7-thienyl-3-quinolinecarbonitriles was prepared. When the thiophene ring was substituted with a water-solubilizing group in a 2,5-, 3,5- or 2,4-pattern, potent inhibition of Src kinase activity was observed. (C) 2002 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(02)00302-5
• 作为产物：
  描述：

  3-噻吩甲醛 在 三氯化铝 、 溴 、 sodium cyanoborohydride 、 溶剂黄146 作用下， 以 乙醇 为溶剂， 生成 4-((5-bromothiophen-3-yl)methyl)morpholine
  参考文献：
  名称：

  Inhibition of Src kinase activity by 4-anilino-7-thienyl-3-quinolinecarbonitriles

  摘要：

  Based on a screening lead from a yeast-based assay to identify Src family kinase inhibitors, a series of 4-anilino-7-thienyl-3-quinolinecarbonitriles was prepared. When the thiophene ring was substituted with a water-solubilizing group in a 2,5-, 3,5- or 2,4-pattern, potent inhibition of Src kinase activity was observed. (C) 2002 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(02)00302-5

文献信息

• 3-cyanoquinolines, 3-cyano-1,6-naphthyridines, and 3-cyano-1,7-naphthyridines as protein kinase inhibitors
  申请人：American Home Products Corporation

  公开号：US20020026052A1

  公开（公告）日：2002-02-28

  This invention provides compounds of Formula (I), having the structure 1 where T, Z, X, A, R 1 , R 2a , R 2b , R 2c , R 3 , R 4 , and n are defined herein, or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of osteoporosis and polycystic kidney disease.

  这项发明提供了具有结构的化合物（I）的公式， 其中T、Z、X、A、R 1 、R 2a 、R 2b 、R 2c 、R 3 、R 4 和n在此处定义，或其药学上可接受的盐，这些化合物可用作抗肿瘤药物，并用于骨质疏松症和多囊肾病的治疗。
• [EN] 3-CYANOQUINOLINES,3-CYANO-1,6-NAPHTHYRIDINES, AND 3-CYANO-1,7-NAPHTHYRIDINES AS PROTEIN KINASE INHIBITORS<br/>[FR] 3-CYANOQUINOLINES,3-CYANO-1,6-NAPHTHYRIDINES ET 3-CYANO-1,7-NAPHTHYRIDINES UTILISEES COMME INHIBITEURS DE PROTEINEKINASE
  申请人：AMERICAN HOME PROD

  公开号：WO2001072711A1

  公开（公告）日：2001-10-04

  Compounds of Formula (I), having the structure or a pharmaceutically salt thereof are useful as antineoplastic agents and in the treatment of osteoporosis and polycystic kidney disease.

  具有结构式（I）或其药物盐的化合物在抗肿瘤药物和治疗骨质疏松症和多囊肾病方面是有用的。
• [EN] SULFONYL BENZAMIDE DERIVATIVES AS BCL-2 INHIBITORS<br/>[FR] DÉRIVÉS DE SULFONYL BENZAMIDE UTILISÉS COMME INHIBITEURS DE BCL-2
  申请人：ASCENTAGE PHARMA SUZHOU CO LTD

  公开号：WO2022161496A1

  公开（公告）日：2022-08-04

  The present disclosure provides compounds having Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein variables are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a disease, disorder, or condition responsive to Bcl-2 protein inhibition, particiularly Bcl-2 WT and/or Bcl-2 G101V.

  本公开提供具有式I的化合物及其药学上可接受的盐和溶剂化物，其中变量如规范中所定义。本公开还提供式I的化合物，用于治疗对Bcl-2蛋白抑制有响应的疾病，失调或情况，特别是Bcl-2 WT和/或Bcl-2 G101V。
• 3-CYANOQUINOLINES,3-CYANO-1,6-NAPHTHYRIDINES, AND 3-CYANO-1,7-NAPHTHYRIDINES AS PROTEIN KINASE INHIBITORS
  申请人：Wyeth

  公开号：EP1268431A1

  公开（公告）日：2003-01-02
• 3-Cyanoquinolines,3-cyano-1,6-naphthyridines, and 3-cyano-1,7-naphthyridines as protein kinase inhibitors
  申请人：Wyeth

  公开号：US20040176602A1

  公开（公告）日：2004-09-09

  This invention provides compounds of Formula (I), having the structure 1 where T, Z, X, A, R 1 , R 2a , R 2b , R 2c , R 3 , R 4 , and n are defined herein, or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of osteoporosis and polycystic kidney disease.