7-methoxy-N-phenyl-6-piperidin-4-yloxyquinazolin-4-amine

• 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: 7-methoxy-N-phenyl-6-piperidin-4-yloxyquinazolin-4-amine
• 化学式: C₂₀H₂₂N₄O₂
• 分子量: 350.4
• InChiKey: MWYGAGALQKZRSP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  26
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  68.3
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• [EN] METHOD FOR PREPARING 1-(4-(4-(3,4-DICHLORO-2-FLUOROPHENYLAMINO)-7-METHOXYQUINAZOLIN-6-YLOXY)PIPERIDIN-1-YL)PROP-2-EN-1-ONE<br/>[FR] PROCÉDÉ DE PRÉPARATION DE 1-(4-(4-(3,4-DICHLORO-2-FLUOROPHÉNYLAMINO)- 7-MÉTHOXYQUINAZOLIN-6-YLOXY)PIPÉRIDIN-1-YL)PROP-2-ÉN-1-ONE
  申请人：HANMI PHARM IND CO LTD

  公开号：WO2014116070A1

  公开（公告）日：2014-07-31

  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-氟苯胺基)-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，通过允许4-(3,4-二氯-2-氟苯胺基)-7-甲氧基喹唑啉-6-醇与N-酰基哌啶衍生物在惰性极性质子溶剂中在碱的存在下反应，实现了更简单的工艺过程。
• 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。
• METHOD FOR PREPARING 1-(4-(4-(3,4-DICHLORO-2-FLUOROPHENYLAMINO)-7-METHOXYQUINAZOLIN-6-YLOXY)PIPERIDIN-1-YL)-PROP-2-EN-1-ONE HYDROCHLORIDE AND INTERMEDIATES USED THEREIN
  申请人：Hanmi Science Co., Ltd.

  公开号：EP2763981B1

  公开（公告）日：2020-01-08
• US20140275534A1
  申请人：——

  公开号：US20140275534A1

  公开（公告）日：2014-09-18