1-[(4-acetyl-2-methoxyphenoxy)methyl]-N-benzyloxycarbonyl-1-aminocyclopropane | 1245794-02-8

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-[(4-acetyl-2-methoxyphenoxy)methyl]-N-benzyloxycarbonyl-1-aminocyclopropane
• 英文别名: benzyl N-[1-[(4-acetyl-2-methoxyphenoxy)methyl]cyclopropyl]carbamate
• CAS: 1245794-02-8
• 化学式: C₂₁H₂₃NO₅
• 分子量: 369.417
• InChiKey: AZYZEIAPFXEOJT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  27
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  73.9
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  1-[(4-acetyl-2-methoxyphenoxy)methyl]-N-benzyloxycarbonyl-1-aminocyclopropane 以56的产率得到1-[(4-acetyl-2-methoxy-5-nitrophenoxy)methyl]-N-benzyloxycarbonyl-1-aminocyclopropane
  参考文献：
  名称：

  Process for the preparation of 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide and synthetic intermediates thereof

  摘要：

  本发明涉及一种制备化合物6-(7-4(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（I）及其药学上可接受的盐的高产率和纯度的方法。该方法相较于先前描述的方法具有各种优点，特别是避免了酰基叠氮中间体及其Curtius重排的使用。还描述了用于制备化合物（I）的新型中间体。

  公开号：

  US08642767B2
• 作为产物：
  描述：

  Cbz-1-氨基环丙烷甲醇 、 香草乙酮 以53.5的产率得到1-[(4-acetyl-2-methoxyphenoxy)methyl]-N-benzyloxycarbonyl-1-aminocyclopropane
  参考文献：
  名称：

  Process for the preparation of 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide and synthetic intermediates thereof

  摘要：

  本发明涉及一种制备化合物6-(7-4(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（I）及其药学上可接受的盐的高产率和纯度的方法。该方法相较于先前描述的方法具有各种优点，特别是避免了酰基叠氮中间体及其Curtius重排的使用。还描述了用于制备化合物（I）的新型中间体。

  公开号：

  US08642767B2

文献信息

• Process for the preparation of 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide and synthetic intermediates thereof
  申请人：Spinelli Silvano

  公开号：US08642767B2

  公开（公告）日：2014-02-04

  A process for the preparation in high yields and purity of the compound 6-(7-4(1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide of formula (I) and of the pharmaceutically acceptable salts thereof is described. The process has various advantages over those previously described, in particular it avoids the use of acyl azide intermediates and their Curtius rearrangement. Novel intermediates useful for the preparation of compound (I) are also described.

  本发明涉及一种制备化合物6-(7-4(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（I）及其药学上可接受的盐的高产率和纯度的方法。该方法相较于先前描述的方法具有各种优点，特别是避免了酰基叠氮中间体及其Curtius重排的使用。还描述了用于制备化合物（I）的新型中间体。
• PROCESS FOR THE PREPARATION OF 6-(7-((1-AMINOCYCLOPROPYL)METHOXY)-6-METHOXYQUINOLIN-4-YLOXY)-N-METHYL-1-NAPHTHAMIDE AND SYNTHETIC INTERMEDIATES THEREOF
  申请人：Spinelli Silvano

  公开号：US20120010415A1

  公开（公告）日：2012-01-12

  A process for the preparation in high yields and purity of the compound 6-(7-4(1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide of formula (I) and of the pharmaceutically acceptable salts thereof is described. The process has various advantages over those previously described, in particular it avoids the use of acyl azide intermediates and their Curtius rearrangement. Novel intermediates useful for the preparation of compound (I) are also described.

  本发明描述了一种制备化合物6-(7-4(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（I）及其药学上可接受的盐的高产率和高纯度的方法。该方法相对于以前描述的方法具有各种优点，特别是避免了使用酰基叠氮中间体及其Curtius重排反应。还描述了用于制备化合物（I）的新型中间体。
• Process for the Preparation of 6-(7-((1-Aminocyclopropyl)Methoxy)-6-Methoxyquinolin-4-Yloxy)-N-Methyl-1-Naphthamide and Synthetic Intermediates Thereof
  申请人：Clovis Oncology Italy S.r.l.

  公开号：US20150191429A1

  公开（公告）日：2015-07-09

  A process for the preparation in high yields and purity of the compound 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide of formula (I) and of the pharmaceutically acceptable salts thereof is described. The process has various advantages over those previously described, in particular it avoids the use of acyl azide intermediates and their Curtius rearrangement. Novel intermediates useful for the preparation of compound (I) are also described.

  本发明提供了一种制备式(I)化合物及其药学上可接受的盐的高产率和高纯度的方法。该方法与先前描述的方法相比具有各种优点，特别是它避免了使用酰基叠氮中间体及其Curtius重排。还描述了用于制备化合物(I)的新型中间体。
• A process for the preparation of 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide and synthetic intermediates thereof
  申请人：EOS Ethical Oncology Science S.p.A. in abbreviated form EOS S.p.A.

  公开号：EP2641897A2

  公开（公告）日：2013-09-25

  A process for the preparation in high yields and purity of the compound 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide of formula (I) and of the pharmaceutically acceptable salts thereof is described. The process has various advantages over those previously described, in particular it avoids the use of acyl azide intermediates and their Curtius rearrangement. Novel intermediates useful for the preparation of compound (I) are also described.

  本发明描述了一种高产率、高纯度制备式（I）化合物 6-(7-((1-氨基环丙基)甲氧基)-6-甲氧基喹啉-4-氧基)-N-甲基-1-萘甲酰胺及其药学上可接受的盐类的工艺。与之前描述的工艺相比，该工艺具有各种优点，尤其是避免了使用酰基叠氮化物中间体及其 Curtius 重排。此外，还描述了用于制备化合物 (I) 的新型中间体。
• INTERMEDIATES FOR THE PREPARATION OF 6-(7-((1-AMINOCYCLOPROPYL)METHOXY)-6-METHOXYQUINOLIN-4-YLOXY)-N-METHYL-1-NAPHTHAMIDE
  申请人：Clovis Oncology Italy S.r.l.

  公开号：EP3103792A1

  公开（公告）日：2016-12-14

  A process for the preparation in high yields and purity of the compound 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide of formula (I) and of the pharmaceutically acceptable salts thereof is described. The process has various advantages over those previously described, in particular it avoids the use of acyl azide intermediates and their Curtius rearrangement. Novel intermediates useful for the preparation of compound (I) are also described.

  本发明描述了一种高产率、高纯度制备式（I）化合物 6-(7-((1-氨基环丙基)甲氧基)-6-甲氧基喹啉-4-氧基)-N-甲基-1-萘甲酰胺及其药学上可接受的盐类的工艺。与之前描述的工艺相比，该工艺具有各种优点，尤其是避免了使用酰基叠氮化物中间体及其 Curtius 重排。此外，还描述了用于制备化合物 (I) 的新型中间体。