tramadol | 152538-36-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: tramadol
• 英文别名: trans-Tramadol；(1R,2S)-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexan-1-ol
• CAS: 152538-36-8
• 化学式: C₁₆H₂₅NO₂
• 分子量: 263.38
• InChiKey: TVYLLZQTGLZFBW-HOCLYGCPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  32.7
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  光气 、 tramadol 以 甲苯 为溶剂， 反应 4.5h， 生成
  参考文献：
  名称：

  一种葛根素曲马多的制备工艺

  摘要：

  本发明公开了一种葛根素曲马多的制备工艺，涉及生物化学技术领域，包括化合物a的氢化还原、化合物b与乙酸酐发生酯化反应、化合物c与对甲氧基苯乙酰氯反应、化合物d的还原反应、化合物e与DMFDMA反应、化合物f还原为葛根素、葛根素曲马多的合成七个工艺过程，本发明合成了一种新的化合物葛根素曲马多，不仅具有与曲马多相当的镇痛效果，且能从根本上减少药物用量，降低药物耐受性与成瘾性，一定程度减缓其对消化系统及循环系统的副作用，控制不良反应,从而实现临床上更加安全有效地用药。

  公开号：

  CN105601625B

文献信息

• Tramadol recovery process
  申请人：IPCA Laboratories Limited

  公开号：EP1785412A1

  公开（公告）日：2007-05-16

  A process for the resolution of isomeric tramadol mixtures comprising: providing a purification stock comprising both cis and trans tramadol; contacting the purification stock with an acid under conditions effective to form an acid salt of the cis and trans tramadol in the purification stock; and separating the cis tramadol acid salt from the trans tramadol to obtain a purified cis tramadol acid salt; and optionally converting the cis tramadol acid salt to cis tramadol or to a pharmaceutically active salt thereof.

  一种用于分离同分异构的曲马多混合物的方法，包括：提供一个包含顺式和反式曲马多的纯化原料；将该纯化原料与酸接触，在有效条件下形成顺式和反式曲马多的酸盐；将顺式曲马多酸盐与反式曲马多分离，获得纯化的顺式曲马多酸盐；可选择将顺式曲马多酸盐转化为顺式曲马多或其药用活性盐。
• [EN] A PROCESS FOR PREPARATION OF O-DESMETHYLTRAMADOL AND SALTS THEREOF<br/>[FR] PROCÉDÉ DE PRÉPARATION DE D'O-DESMÉTHYLTRAMADOL ET DE SELS DE CELUI-CI
  申请人：R L FINE CHEM PRIVATE LTD

  公开号：WO2019053494A1

  公开（公告）日：2019-03-21

  The present invention relates to a process of preparation of O-Desmethyl tramadol through potassium hydroxide mediated demethylation of Tramadol under phase transfer conditions.

  本发明涉及一种通过钾氢氧化物介导的相转移条件下的曲马多去甲基化制备O-去甲基曲马多的方法。
• Delivery of analgesics through an inhalation route
  申请人：——

  公开号：US20030017117A1

  公开（公告）日：2003-01-23

  The present invention relates to the delivery of analgesics through an inhalation route. Specifically, it relates to aerosols containing acetaminophen, orphenadrine or tramadol that are used in inhalation therapy. In a composition aspect of the present invention, the aerosol comprises particles comprising at least 5 percent by weight of acetaminophen, orphenadrine or tramadol. In a method aspect of the present invention, one of acetaminophen, orphenadrine or tramadol is delivered to a mammal through an inhalation route. The method comprises: a) heating a composition, wherein the composition comprises at least 5 percent by weight of acetaminophen, orphenadrine or tramadol, to form a vapor; and, b) allowing the vapor to cool, thereby forming a condensation aerosol comprising particles, which is inhaled by the mammal. In a kit aspect of the present invention, a kit for delivering acetaminophen, orphenadrine or tramadol through an inhalation route to a mammal is provided which comprises: a) a composition comprising at least 5 percent by weight of acetaminophen, orphenadrine or tramadol; and, b) a device that forms an acetaminophen, orphenadrine or tramadol containing aerosol from the composition, for inhalation by the mammal.

  本发明涉及通过吸入途径传递镇痛剂。具体而言，涉及含有对乙酰氨基酚、奥芬那定或曲马多的气溶胶，用于吸入疗法。在本发明的组成方面，气溶胶包括至少占重量5%的对乙酰氨基酚、奥芬那定或曲马多的颗粒。在本发明的方法方面，通过吸入途径将对乙酰氨基酚、奥芬那定或曲马多之一传递给哺乳动物。该方法包括：a）加热组合物，其中组合物至少包括占重量5%的对乙酰氨基酚、奥芬那定或曲马多，以形成蒸气;和，b）允许蒸汽冷却，从而形成被哺乳动物吸入的凝结气溶胶颗粒。在本发明的套件方面，提供了一种用于通过吸入途径向哺乳动物传递对乙酰氨基酚、奥芬那定或曲马多的套件，该套件包括：a）含有至少占重量5%的对乙酰氨基酚、奥芬那定或曲马多的组合物;和，b）用于从组合物中形成含有对乙酰氨基酚、奥芬那定或曲马多的气溶胶，供哺乳动物吸入的装置。
• Adduct of topiramate and tramadol hydrochioride and uses thereof
  申请人：Cilag AG

  公开号：EP1364649A1

  公开（公告）日：2003-11-26

  This invention relates to a new pharmaceutically useful compound which is a stoichiometrically 1:1 adduct of tramadol hydrochloride and topiramate, to the manufacture and use thereof.

  本发明涉及一种新的药用化合物，它是盐酸曲马多和托吡酯按1:1的比例加成的化合物，并涉及其制造和使用。
• PHARMACEUTICAL COMPOSITIONS COMBINING ANALGESICS AND ANTICONVULSANT AGENTS FOR THE TREATMENT OF CHRONIC AND ACUTE PAIN
  申请人：ESPINOZA ABDALA, Leopoldo de Jesús

  公开号：EP1944022A1

  公开（公告）日：2008-07-16

  The present invention relates to pharmaceutical industry in general, and to pharmaceutical industry making medicaments for treatment of conditions of sharp and chronic pain. The composition is characterized in that it comprises a combination of an analgesic and an anticonvulsant, wherein the analgesic is known as Tramadol and the anticonvu.lsant drug is known as Gabapentin, wherein Tramadol is present in a rate with respect to the total weight of the formulation of from 3 to 8.3% and Gabapentin is present in a rate with respect to the total weight of the formulation of from 16 to 83%.

  本发明涉及一般制药工业，以及制造治疗剧痛和慢性疼痛药物的制药工业。 该组合物的特征在于它包括镇痛药和抗惊厥药的组合，其中镇痛药称为曲马多，抗惊厥药称为加巴喷丁，其中曲马多的含量占制剂总重量的 3%至 8.3%，加巴喷丁的含量占制剂总重量的 16%至 83%。