1-(4-((7-methoxy-4-(phenylamino)quinazolin-6-yl)oxy)piperidin-1-yl)prop-2-en-1-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 1-(4-((7-methoxy-4-(phenylamino)quinazolin-6-yl)oxy)piperidin-1-yl)prop-2-en-1-one
• 英文别名: 1-(4-((7-Methoxy-4-(phenylamino)quinazolin-6-yl)oxy)piperidin-1-yl)prop-2-en-1-one；1-[4-(4-anilino-7-methoxyquinazolin-6-yl)oxypiperidin-1-yl]prop-2-en-1-one
• 化学式: C₂₃H₂₄N₄O₃
• 分子量: 404.469
• InChiKey: GYOZIRHAFXZCRS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  30
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  76.6
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• [EN] HETEROCYCLIC INHIBITORS OF TYROSINE KINASE<br/>[FR] INHIBITEURS HÉTÉROCYCLIQUES DE TYROSINE KINASE
  申请人：UNIV TEXAS

  公开号：WO2020219904A1

  公开（公告）日：2020-10-29

  The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of HER2 or EGFR for the treatment or prevention of disease, including cancer.

  本公开涉及杂环化合物和方法，这些方法可能作为HER2或EGFR的抑制剂，用于治疗或预防疾病，包括癌症。
• Method For Preparing 1-(4-(4-(3,4-Dichloro-2-Fluorophenylamino)-7-Methoxyquinazolin-6-Yloxy)Piperidin-1-Yl)Prop-2-En-1-One
  申请人：HANMI PHARM. CO., LTD.

  公开号：US20150344458A1

  公开（公告）日：2015-12-03

  The present invention relates to a novel method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)prop-2-en-1-one in a simpler process as compared with conventional methods by allowing 4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-ol to react with an N-acyl piperidine derivative in an inert polar protic solvent in the presence of a base.

  本发明涉及一种新型制备1-(4-(4-(3,4-二氯-2-氟苯基氨基)-7-甲氧基喹唑啉-6-氧基)哌啶-1-基)丙-2-烯-1-酮的方法，与传统方法相比，该方法更简单，通过在惰性极性质溶剂中加入碱使4-(3,4-二氯-2-氟苯基氨基)-7-甲氧基喹唑啉-6-醇与N-酰基哌啶衍生物反应。
• METHOD FOR PREPARING 1-(4-(4-(3,4-DICHLORO-2-FLUOROPHENYLAMINO)-7-METHOXYQUINAZOLIN-6-YLOXY)PIPERIDIN-1-YL)-PROP-2-EN-1-ONE
  申请人：Hanmi Science Co., Ltd.

  公开号：EP3611172A1

  公开（公告）日：2020-02-19

  The present invention relates to an improved method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-prop-2-en-1-one, which selectively and effectively inhibits the growth of cancer cells induced by over-expression of an epidermal growth factor receptor (EGFR) and prevents the development of drug resistance caused by mutation of a tyrosine kinase.

  本发明涉及一种制备 1-(4-(4-(3,4-二氯-2-氟苯基氨基)-7-甲氧基喹唑啉-6-基氧基)哌啶-1-基)-丙-2-烯-1-酮的改进方法，该方法可选择性地有效抑制表皮生长因子受体（EGFR）过度表达所诱导的癌细胞的生长，并防止因酪氨酸激酶突变而产生的耐药性。
• Heterocyclic inhibitors of tyrosine kinase
  申请人：Board of Regents, The University of Texas System

  公开号：US11365189B2

  公开（公告）日：2022-06-21

  The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of HER2 or EGFR for the treatment or prevention of disease, including cancer.

  本公开涉及可用作 HER2 或表皮生长因子受体抑制剂用于治疗或预防疾病（包括癌症）的杂环化合物和方法。
• US20140275534A1
  申请人：——

  公开号：US20140275534A1

  公开（公告）日：2014-09-18