6alpha-氯-7,8-二去氢-4,5alpha-环氧-17-甲基吗喃-3-醇 | 63783-53-9

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 吗啡烷
• 中文名称: 6alpha-氯-7,8-二去氢-4,5alpha-环氧-17-甲基吗喃-3-醇
• 英文名称: Chloromorphide
• 英文别名: (4R,4aR,7S,7aR,12bS)-7-chloro-3-methyl-2,4,4a,7,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-9-ol
• CAS: 63783-53-9
• 化学式: C₁₇H₁₈ClNO₂
• 分子量: 303.8
• InChiKey: URUOTSLJEBANHA-ZFDIKFDDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  21
• 可旋转键数：
  0
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  32.7
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• METHODS AND COMPOSITIONS FOR PREVENTING OPIOID ABUSE
  申请人：Waterville Valley Technologies, Inc.

  公开号：US20160326182A1

  公开（公告）日：2016-11-10

  Abuse-resistant opioid compounds, drug delivery systems, pharmaceutical compositions comprising an opioid covalently bound to a chemical moiety are provided. Methods of delivering an active ingredient to a subject and methods of preventing opioid abuse are also provided.

  提供了耐滥用的阿片类化合物、药物输送系统、含有阿片类药物与化学基团共价结合的制药组合物。还提供了将活性成分输送给受试者的方法以及预防阿片类药物滥用的方法。
• [EN] COMPOSITIONS AND METHODS FOR THE TREATMENT OF PAIN AND DEPENDANCE DISORDERS<br/>[FR] COMPOSITIONS ET MÉTHODES DE TRAITEMENT DE LA DOULEUR ET DE TROUBLES DE LA DÉPENDANCE
  申请人：RIPPLE THERAPEUTICS CORP

  公开号：WO2021024039A1

  公开（公告）日：2021-02-11

  Provided herein are (e.g., controlled release) compositions for the treatment of acute or chronic diseases or disorders. Described herein are processable opioid conjugates. Also described herein are compositions and methods for the treatment of central nervous system (CNS) diseases or disorders including chronic pain (e.g., cancer pain), acute pain, opioid addiction, alcohol addiction, alcohol dependence, opioid-induced constipation, and narcotic depression. Said compositions and methods comprise opioid agonists and/or opioid antagonists, which demonstrate CNS activity and/or other desirable activities. Injection of said compositions subcutaneously or intraspinally provides therapeutic benefit to individuals suffering from CNS diseases or disorders

  本文提供了用于治疗急性或慢性疾病或障碍的（例如，控释）组合物。本文描述了可加工的阿片类结合物。本文还描述了用于治疗中枢神经系统（CNS）疾病或障碍的组合物和方法，包括慢性疼痛（例如，癌症疼痛）、急性疼痛、阿片类成瘾、酒精成瘾、酒精依赖、阿片类引起的便秘和麻醉性抑郁症。所述组合物和方法包括表现出CNS活性和/或其他理想活性的阿片类激动剂和/或阿片类拮抗剂。将所述组合物皮下或脊髓内注射可为患有中枢神经系统疾病或障碍的个体提供治疗益处。
• [EN] FACILE 'ONE POT' PROCESS FOR APOMORPHINE FROM CODEINE<br/>[FR] PROCÉDÉ EN RÉCIPIENT UNIQUE, FACILE, POUR PRODUIRE DE L'APOMORPHINE À PARTIR DE LA CODÉINE
  申请人：MALLINCKRODT INC

  公开号：WO2009038958A1

  公开（公告）日：2009-03-26

  An improved method for producing apomorphine and derivatives thereof is provided. The method is a convenient 'one-pot' process, comprising the conversion of codeine into apomorphine without isolating the apocodeine intermediate. Use of water reactive scavengers, reagents that will react irreversibly with water, decreases side product formation and allows the use of milder reaction conditions. This one-pot synthesis of apomorphine from codeine provides a faster reaction with improved yields at temperatures lower as compared to conventional methods. The lower operating temperatures and less volatile reactants make the method particularly useful for large-scale manufacturing.

  提供了一种改进的制备阿波莫啡和其衍生物的方法。该方法是一种便利的“一锅法”过程，包括将可待因转化为阿波莫啡而无需分离阿波可待因中间体。使用对水具有反应性的清除剂，即会与水不可逆反应的试剂，可减少副产物的形成，并允许使用较温和的反应条件。与传统方法相比，从可待因合成阿波莫啡的这种一锅法合成提供了更快的反应速度和更高的产率，且在较低温度下进行。较低的操作温度和较不挥发的反应物使该方法特别适用于大规模制造。
• Process for Making Apomorphine and Apocodeine
  申请人：Gurusamy Narayanasamy

  公开号：US20100228032A1

  公开（公告）日：2010-09-09

  There is provided an improved and convenient process for the synthesis of aporphines, such as apomorphine and apocodeine, by the rearrangement of the corresponding morphine or codeine derivatives. The use of a suitable water scavenger in an acid catalyzed rearrangement of the morphine derivatives unexpectedly results in a reaction temperature convenient for plant operation without sacrificing product. The method of the present invention also alleviates the cumbersome operations that were employed in the prior art to eliminate water from the reaction mixture at the elevated temperatures. This process is adaptable for the general preparation of other aporphines from the corresponding morphine congeners.

  提供了一种改进和便利的合成阿泼吗啡(apomorphine)和阿泼可定(apocodeine)等阿泼啡(aporphines)的方法，该方法通过对应的吗啡(morphine)或可待因(codeine)衍生物的重排来实现。在酸催化的吗啡衍生物重排中使用适当的水清除剂，出乎意料地得到了适合植物操作的反应温度，而不会牺牲产品。本发明方法还减轻了在先前的技术中用于在高温下从反应混合物中消除水的繁琐操作。该过程适用于从相应的吗啡同系物中普遍制备其他阿泼啡的方法。
• Facile "One Pot' Process for Apomorphine From Codeine
  申请人：Gurusamy Narayanasamy

  公开号：US20100216998A1

  公开（公告）日：2010-08-26

  An improved method for producing apomorphine and derivatives thereof is provided. The method is a convenient ‘one-pot’ process, comprising the conversion of codeine into apomorphine without isolating the apocodeine intermediate. Use of water reactive scavengers, reagents that will react irreversibly with water, decreases side product formation and allows the use of milder reaction conditions. This one-pot synthesis of apomorphine from codeine provides a faster reaction with improved yields at temperatures lower as compared to conventional methods. The lower operating temperatures and less volatile reactants make the method particularly useful for large-scale manufacturing.

  提供了一种改进的制备阿泼吗啡及其衍生物的方法。该方法是一种方便的“一锅法”过程，包括将可待因转化为阿泼吗啡而不需要分离出阿泼可待因中间体。使用水反应性清除剂，即会与水不可逆反应的试剂，可减少副产物的形成并允许使用较温和的反应条件。与传统方法相比，从可待因合成阿泼吗啡的这种一锅法合成提供了更快的反应速度和更高的产量，且操作温度更低，反应物更不易挥发。这种方法特别适用于大规模制造。