5-[(1R)-2-bromo-1-(1-butoxyethoxy)ethyl]-8-butoxy-1H-quinolin-2-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 5-[(1R)-2-bromo-1-(1-butoxyethoxy)ethyl]-8-butoxy-1H-quinolin-2-one
• 化学式: C₂₁H₃₀BrNO₄
• 分子量: 440.4
• InChiKey: ZEZUGWLHEYSBMM-FUBQLUNQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  27
• 可旋转键数：
  12
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  56.8
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] METHODS FOR THE PREPARATION OF INDACATEROL AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF<br/>[FR] PROCÉDÉS DE PRÉPARATION D'INDACATÉROL ET DE SES SELS PHARMACEUTIQUEMENT ACCEPTABLES
  申请人：CRYSTAL PHARMA SA

  公开号：WO2014044288A1

  公开（公告）日：2014-03-27

  The invention relates to new and improved processes for the preparation of Indacaterol and pharmaceutically acceptable salts thereof as well as intermediates for the preparation of Indacaterol. The new process avoids the use of the epoxide compound known in the art and the impurities associated therewith and results in a higher yield.

  该发明涉及制备Indacaterol及其药用可接受盐的新的和改进的工艺，以及制备Indacaterol的中间体。新工艺避免了在艺术中已知的环氧化合物的使用及相关的杂质，并且产量更高。
• [EN] METHODS FOR THE PREPARATION OF INDACATEROL AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF<br/>[FR] PROCÉDÉS DE PRÉPARATION D'INDACATÉROL ET DE SELS PHARMACEUTIQUEMENT ACCEPTABLES DE CELUI-CI
  申请人：CRYSTAL PHARMA SAU

  公开号：WO2014044566A1

  公开（公告）日：2014-03-27

  The invention relates to new and improved processes for the preparation of Indacaterol and pharmaceutically acceptable salts thereof as well as intermediates for the preparation of Indacaterol. The new process avoids the use of the epoxide compound known in the art and the impurities associated therewith and results in a higher yield.

  该发明涉及一种新的改进工艺，用于制备Indacaterol及其药用可接受的盐，以及用于制备Indacaterol的中间体。这种新工艺避免了在现有技术中已知的环氧化合物的使用以及相关的杂质，并且产率更高。
• METHODS FOR THE PREPARATION OF INDACATEROL AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
  申请人：CRYSTAL PHARMA S.A.U.

  公开号：US20150225346A1

  公开（公告）日：2015-08-13

  The invention relates to new and improved processes for the preparation of Indacaterol and pharmaceutically acceptable salts thereof as well as intermediates for the preparation of Indacaterol. The new process avoids the use of the epoxide compound known in the art and the impurities associated therewith and results in a higher yield.

  本发明涉及制备Indacaterol及其药用可接受盐的新的和改进的工艺，以及制备Indacaterol的中间体。新的工艺避免了在艺术中已知的环氧化合物及其相关杂质的使用，并且产量更高。
• INDACATEROL FREE BASE IN SOLID FORM
  申请人：Crystal Pharma, S.A.U.

  公开号：EP3138837A1

  公开（公告）日：2017-03-08

  The present invention relates to the Indacaterol free base in solid form. The Indacataterol free base may be in a crystalline form or in an amorphous form. The present invention also discloses an improved preparation of the Idacaterol maleate salt using the isolated Indacaterol free base in solid form as an intermediate. Indacataterol (5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxyethyl]-8-hydroxy-(1H)-quinolin-2-one) is a beta-selective adrenoceptor agonists with a potent bronchodilating activity. Indacaterol is especially useful for the treatment of asthma and chronic obstructive pulmonary disease (COPD) and is sold commercially as the maleate salt.

  本发明涉及固体形式的茚达特罗游离基。茚达特罗游离碱可以是结晶形式或无定形形式。 本发明还公开了一种以分离的固体形式的茚达特罗游离碱为中间体制备马来酸茚达特罗盐的改进方法。 茚达特罗（5-[(R)-2-(5,6-二乙基-茚满-2-基氨基)-1-羟乙基]-8-羟基-(1H)-喹啉-2-酮）是一种β选择性肾上腺素受体激动剂，具有强效的支气管扩张活性。茚达特罗尤其适用于治疗哮喘和慢性阻塞性肺病（COPD），以马来酸盐的形式进行商业销售。
• PROCESS FOR THE PREPARATION OF INDACATEROL AND INTERMEDIATES THEREOF
  申请人：Crystal Pharma S.A.U

  公开号：EP2897937B1

  公开（公告）日：2017-12-06