donepezil monoacetic acid salt | 942424-78-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: donepezil monoacetic acid salt
• 英文别名: donepezil acetate；donepesil acetate；Acetic acid;2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one
• CAS: 942424-78-4
• 化学式: C₂H₄O₂*C₂₄H₂₉NO₃
• 分子量: 439.552
• InChiKey: QBLQVELKNHBOSX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.45
• 重原子数：
  32
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  76.1
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• POLYMORPHS OF DONEPEZIL SALTS, PREPARATION METHODS AND USES THEREOF
  申请人：Zhang Hesheng

  公开号：US20100311793A1

  公开（公告）日：2010-12-09

  Preparation methods of mesylate, para-toluenesulfonate, succinate, tartrate, sulphate, nitrate, phosphate, salicylate, fumarate, maleate, gallate, acetylsalicylate, benzenesulphonate, citrate, aspartate, glutaminate, lactate, gluconate, ascorbate, malonate, malate, sorbate, acetate or formate of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine (i.e., Donepezil). Novel polymorphs formed from these salts and their preparation methods. Co-crystals formed from Donepezil hydrochloride and maleic acid, fumaric acid, citric acid, salicylic acid, tartaric acid or succinic acid.

  1-苄基-4-[(5,6-二甲氧基-1-茚酮)-2-基]甲基哌啶（即多奈哌齐）的甲磺酸盐、对甲苯磺酸盐、琥珀酸盐、酒石酸盐、硫酸盐、硝酸盐、磷酸盐、水杨酸盐、富马酸盐、马来酸盐、没食子酸盐、乙酰水杨酸盐、苯磺酸盐、柠檬酸盐、天冬氨酸盐、谷氨酸盐、乳酸盐、葡萄糖酸盐、抗坏血酸盐、丙二酸盐、苹果酸盐、山梨酸盐、乙酸盐或甲酸盐的制备方法。从这些盐中形成的新型多晶形态及其制备方法。由多奈哌齐盐酸盐和马来酸、富马酸、柠檬酸、水杨酸、酒石酸或琥珀酸形成的共晶体。
• Novel Process for Production of Highly Pure Polymorph (I) Donepezil Hydrochloride
  申请人：Neu Jozsef

  公开号：US20080306271A1

  公开（公告）日：2008-12-11

  The present invention provides a novel, industrially realizable and economically preferable process for production of highly pure 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methyl piperidine hydrochloride, i.e., donepezil hydrochloride shown in the following reaction scheme, in Polymorph (I) morphological crystal form. (I) In one of the key steps of the process, during the hydrogenation 5,6-dimethoxy 2-(pyridine-4-yhnethylene)indan- 1 -one hydrochloride is saturated using Pd carbon to get 4-[(5,6-dimethoxy- 1 -indanon)-2-yl]-methyl piperidine at more than 97% HPLC purity. In the crystallization step donepezil-hydrochloride is crystallized from an aqueous alcoholic solvent to get Polymorph (I) in at least 99.95% HPLC purity.

  本发明提供了一种新颖的、可在工业上实现的、经济上优选的过程，用于生产高纯度的1-苄基-4-[(5,6-二甲氧基-1-吲哚酮)-2-基]甲基哌啶盐酸盐，即多奈哌齐盐酸盐，以Polymorph (I)形态晶体形式呈现在以下反应方案中。在该过程的关键步骤之一中，在氢化过程中，使用Pd碳饱和5,6-二甲氧基2-(吡啶-4-基亚乙烯基)吲哚-1-酮盐酸盐以获得在97%以上的HPLC纯度下的4-[(5,6-二甲氧基-1-吲哚酮)-2-基]甲基哌啶。在结晶步骤中，多奈哌齐盐酸盐从水醇溶剂中结晶出来，以至少99.95%的HPLC纯度得到Polymorph (I)。
• DONEPEZIL DERIVATIVE AND USE THEREOF
  申请人：NORATECH PHARMACEUTICALS, INC.

  公开号：US20170319561A1

  公开（公告）日：2017-11-09

  The present invention relates to a donepezil derivative of general formula (I) or a pharmaceutically acceptable salt thereof, wherein R in the formula is as disclosed herein; and a method for preparation thereof; and a composition comprising an effective amount of a compound of the general formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to use of a compound of the general formula (I) or a pharmaceutically acceptable salt thereof in preparing a medicament for treating a disease resulted from an abnormality in acetylcholinesterase activity.

  本发明涉及一种通式(I)的多奈哌齐衍生物或其药学上可接受的盐，其中公式中的R如本文所述；以及其制备方法；以及包含通式(I)的化合物或其药学上可接受的盐的有效量的组合物。本发明还涉及使用通式(I)的化合物或其药学上可接受的盐制备治疗由乙酰胆碱酯酶活性异常引起的疾病的药物。
• Donepezil derivative and use thereof
  申请人：NORATECH PHARMACEUTICALS, INC.

  公开号：US10080746B2

  公开（公告）日：2018-09-25

  The present invention relates to a donepezil derivative of general formula (I) or a pharmaceutically acceptable salt thereof, wherein R in the formula is as disclosed herein; and a method for preparation thereof; and a composition comprising an effective amount of a compound of the general formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to use of a compound of the general formula (I) or a pharmaceutically acceptable salt thereof in preparing a medicament for treating a disease resulted from an abnormality in acetylcholinesterase activity.

  本发明涉及通式(I)的多奈哌齐衍生物或其药学上可接受的盐，其中式中的R如本文所公开；及其制备方法；以及包含有效量的通式(I)化合物或其药学上可接受的盐的组合物。本发明还涉及通式（I）化合物或其药学上可接受的盐在制备治疗乙酰胆碱酯酶活性异常导致的疾病的药物中的用途。
• NOVEL PROCESS FOR PRODUCTION OF HIGHLY PURE POLYMORPH (I) DONEPEZIL HYDROCHLORIDE
  申请人：Richter Gedeon NYRT

  公开号：EP1966136A2

  公开（公告）日：2008-09-10