(4-methoxyphenyl)methyl N-cyclopropyl-N-(hydroxymethyl)carbamate

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (4-methoxyphenyl)methyl N-cyclopropyl-N-(hydroxymethyl)carbamate
• 化学式: C₁₃H₁₇NO₄
• 分子量: 251.28
• InChiKey: VKHQXJPRHMKUIU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  18
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  59
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] PROCESS FOR PREPARING THE ANTI-TUMOR AGENT 6-(7-((1-AMINOCYCLOPROPYL) METHOXY)-6-METHOXYQUINOLIN-4-YLOXY)-N-METHYL-1-NAPHTHAMIDE AND ITS CRYSTALLINE<br/>[FR] PROCÉDÉ POUR L'ÉLABORATION D'UN AGENT ANTITUMORAL, LA 6-(7-((1-AMINO-CYCLO-PROPYL)-MÉTHOXY)-6- MÉTHOXYQUINOLIN-4-YLOXY)-N-MÉTHYL-1-NAPHTHAMIDE,ET DE SA FORME CRISTALLINE
  申请人：ADVENCHEN PHARMACEUTICALS LLC

  公开号：WO2014113616A1

  公开（公告）日：2014-07-24

  The present invention relates a new process to synthesize 6-(7-((l-aminocyclo-propyl)- methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl- l -naphthamide (AL3810) by deprotection of substituted benzyl 1 -((6-methoxy-4-(5-(methylcarbamoyl)naphthalen-2-yloxy)quinolin-7-yloxy)- methyl)cyc-lopropylcarbamate (Formula I) under a diluted or weak acidic condition. A stable crystalline form of 6-(7-((l-aminocyclo-propyl)-methoxy)-6-methoxyquinolin-4-yloxy)-N- methyl- 1 -naphthamide has also been prepared.

  本发明涉及一种新的合成过程，通过在稀释或弱酸性条件下去保护取代苄基1-((6-甲氧基-4-(5-(甲基氨甲酰)萘-2-氧基)喹啉-7-氧基)-甲基)环丙基氨基甲酸酯（化学式I），合成6-(7-((1-氨基环丙基)-甲氧基)-6-甲氧基喹啉-4-氧基)-N-甲基-1-萘酰胺（AL3810）通过脱保护。同时还制备了6-(7-((1-氨基环丙基)-甲氧基)-6-甲氧基喹啉-4-氧基)-N-甲基-1-萘酰胺的稳定晶型。
• [EN] PROCESS FOR PREPARING AN ANTI-CANCER AGENT, 1-((4-(4-FLUORO-2-METHYL-1H-INDOL-5-YLOXY)-6-METHOXYQUINOLIN-7-YLOXY)METHYL) CYCLOPROPANAMINE, ITS CRYSTALLINE FORM AND ITS SALTS<br/>[FR] PROCÉDÉ DE PRÉPARATION D'UN AGENT ANTICANCÉREUX 1-((4-(4-FLUORO-2-MÉTHYL-1H-INDOL-5-YLOXY)-6-MÉTHOXYQUINOLINE-7-YLOXY)MÉTHYL) CYCLOPROPANAMINE, SA FORME CRISTALLINE ET SES SELS
  申请人：ADVENCHEN PHARMACEUTICALS LLC

  公开号：WO2016179123A1

  公开（公告）日：2016-11-10

  The present invention relates a new process to synthesize 1-((4-(4-Fluoro-2-methyl-1H- indol-5-yloxy)-6-methoxyquinolin-7-yloxy)methyl)cyclopropanamine (AL3818). A stable crystalline form of A13818 has been prepared. Salts and their crystalline forms of AL3818 have been also prepared. Anti-cancer and optometric activities of AL3818 and its salts have been further tested. New process has been outlined in Scheme I.

  本发明涉及一种合成1-((4-(4-氟-2-甲基-1H-吲哚-5-氧基)-6-甲氧基喹啉-7-氧基)甲基)环丙胺（AL3818）的新工艺。已制备了一种稳定的晶体形式的A13818。同时，还制备了AL3818盐及其晶体形式。对AL3818及其盐的抗癌和眼科活性进行了进一步测试。新工艺已在方案I中概述。
• PROCESS FOR PREPARING THE ANTI-TUMOR AGENT 6-(7-((1-AMINOCYCLOPROPYL) METHOXY)-6-METHOXYQUINOLIN-4-YLOXY)-N-METHYL-1-NAPHTHAMIDE AND ITS CRYSTALLINE
  申请人：Advenchen Pharmaceuticals LLC

  公开号：EP2945931A1

  公开（公告）日：2015-11-25
• PROCESS FOR PREPARING AN ANTI-CANCER AGENT, 1-((4-(4-FLUORO-2-METHYL-1H-INDOL-5-YLOXY)-6-METHOXYQUINOLIN-7-YLOXY)METHYL) CYCLOPROPANAMINE, ITS CRYSTALLINE FORM AND ITS SALTS
  申请人：Advenchen Pharmaceuticals LLC

  公开号：EP3291814A1

  公开（公告）日：2018-03-14