7,8,9,10-tetrahydro-8-methyl-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine | 328055-92-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 英文名称: 7,8,9,10-tetrahydro-8-methyl-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine
• 英文别名: 14-methyl-5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca-2(11),3,5,7,9-pentaene；8-Methyl-7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline；14-methyl-5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca-2,4,6,8,10-pentaene
• CAS: 328055-92-1
• 化学式: C₁₄H₁₅N₃
• 分子量: 225.293
• InChiKey: NJHXRPHFYMFVFC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  17
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  29
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• Process for Preparing Quinoxaline Derivatives
  申请人：SOLDEVILLA MADRID Nuria

  公开号：US20120004239A1

  公开（公告）日：2012-01-05

  The present invention provides an improved process for preparing a compound of formula (IIIA), an intermediate of the synthesis of varenicline. Also, the present invention provides an improved process for preparing varenicline, or a pharmaceutically acceptable salt or solvate thereof. Furthermore, the present invention provides a process for decolorizing varenicline, or a salt or solvate thereof. Still further, the present invention provides a process of preparing varenicline L-tartrate with improved yield. Still further, the present invention relates to the use of compound of formula (V), or a salt or solvate thereof, as a reference marker and reference standard for assessing the purity of varenicline, or a salt or solvate thereof.

  本发明提供了一种改进的制备式（IIIA）化合物的方法，该化合物是瓦伦尼克林合成的中间体。此外，本发明提供了一种改进的制备瓦伦尼克林或其药学上可接受的盐或溶剂的方法。此外，本发明提供了一种脱色瓦伦尼克林或其盐或溶剂的方法。此外，本发明还提供了一种制备瓦伦尼克林-L-酒石酸盐的方法，其收率得到了改善。此外，本发明涉及使用式（V）化合物或其盐或溶剂作为参考标记和参考标准来评估瓦伦尼克林或其盐或溶剂的纯度。
• Cocrystal of varenicline and oxalic acid, pharmaceutical composition thereof, and methods of use thereof
  申请人：Almatica Pharma LLC

  公开号：US11040983B1

  公开（公告）日：2021-06-22

  Provided is a cocrystal of varenicline and oxalic acid. In particular, provided is a cocrystal of varenicline and oxalic acid of formula (I) having a molar ratio of varenicline to oxalic acid of 1:1.5. Also provided is a process for preparing the cocrystal, a pharmaceutical composition containing the cocrystal and a method of using the cocrystal and pharmaceutical composition, such as for reducing nicotine addiction or tobacco use.

  提供的是瓦伦尼克林和草酸的共晶体。特别地，提供的是瓦伦尼克林和草酸的共晶体，其化学式为(I)，瓦伦尼克林与草酸的摩尔比为1:1.5。还提供了制备该共晶体的方法，含有该共晶体的制药组合物以及使用该共晶体和制药组合物的方法，例如用于减少尼古丁成瘾或烟草使用。
• PREPARATION OF SUBSTITUTED QUINOXALINES FROM THE DIANILINE WITH 2,3-DIHYDROXY-1,4-DIOXANE
  申请人：Pfizer Products Inc.

  公开号：EP1638971B1

  公开（公告）日：2008-08-20
• MULTI-API LOADING PRODRUGS
  申请人：Alkermes Pharma Ireland Limited

  公开号：EP2655314B1

  公开（公告）日：2018-02-07
• Methods of Reducing Degradant Formation in Pharmaceutical Compositions of Varenicline
  申请人：Waterman C. Kenneth

  公开号：US20080026059A1

  公开（公告）日：2008-01-31

  The invention relates to methods for reducing degradant formation in pharmaceutical dosage forms of varenicline, which are useful for aiding smoking cessation and which have good storage stability. In particular, the present invention relates to methods for preparing formulations of varenicline wherein the dosage forms that are produced therefrom generate under specified storage conditions less than about 4% on a weight basis of the N-formyl and N-methyl degradation products.