(4R,4aR,7S,7aR,12bS)-3-methyl-2,4,4a,7,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7,9-diol;methanol;sulfuric acid

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 吗啡烷
• 英文名称: (4R,4aR,7S,7aR,12bS)-3-methyl-2,4,4a,7,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7,9-diol;methanol;sulfuric acid
• 化学式: C18H25NO8S
• 分子量: 415.5
• InChiKey: INDKSDKNVXNLLZ-ZGZIUUKVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.15
• 重原子数：
  28
• 可旋转键数：
  0
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  156
• 氢给体数：
  5
• 氢受体数：
  9

文献信息

• Morphine Sulfate Methanolic Solvate, Processes for Making Same and Related Compositions and Methods for Treating Pain
  申请人：Johnson Matthey Public Limited Company

  公开号：US20150361084A1

  公开（公告）日：2015-12-17

  Processes for reducing the amount of impurities, especially α,β-unsaturated ketones (ABUK), in materials containing morphine. Novel compounds, namely low ABUK morphine sulfate methanolic solvate, and a novel crystal form are also described. The method for making morphine sulfate methanolic solvate comprises mixing a morphine free base composition with methanol to form a solution and adding a liquid comprising sulfuric acid to the solution to form a morphine sulfate methanolic solvate precipitate. A method of making a morphine sulfate compound comprises drying the morphine sulfate methanolic solvate in the presence of water vapor, such that methanol molecules are removed and replaced with water vapor molecules. A composition for treating pain comprises the morphine sulfate compound and at least one pharmaceutically acceptable excipient. A method for treating pain comprises administering to a patient in need thereof the composition comprising the morphine sulfate compound and at least one pharmaceutically acceptable excipient.

  减少含有吗啡材料中杂质，特别是α，β-不饱和酮（ABUK）的过程。还描述了新的化合物，即低ABUK吗啡硫酸盐甲醇溶剂和新的晶体形式。制备吗啡硫酸盐甲醇溶剂的方法包括将吗啡自由碱组成物与甲醇混合形成溶液，并向溶液中加入含硫酸的液体，以形成吗啡硫酸盐甲醇溶剂沉淀。制备吗啡硫酸盐化合物的方法包括在水蒸气存在下干燥吗啡硫酸盐甲醇溶剂，使甲醇分子被去除并被水蒸气分子替换。用于治疗疼痛的组合物包括吗啡硫酸盐化合物和至少一种药用可接受的赋形剂。治疗疼痛的方法包括向需要该组合物的患者施用包含吗啡硫酸盐化合物和至少一种药用可接受的赋形剂的组合物。
• MORPHINE SULFATE METHANOLIC SOLVATE, PROCESSES FOR MAKING SAME AND RELATED COMPOSITIONS AND METHODS FOR TREATING PAIN
  申请人：Johnson Matthey Public Limited Company

  公开号：EP2970320A2

  公开（公告）日：2016-01-20
• US20140275146A1
  申请人：——

  公开号：US20140275146A1

  公开（公告）日：2014-09-18
• US9127008B2
  申请人：——

  公开号：US9127008B2

  公开（公告）日：2015-09-08
• [EN] MORPHINE SULFATE METHANOLIC SOLVATE, PROCESSES FOR MAKING SAME AND RELATED COMPOSITIONS AND METHODS FOR TREATING PAIN<br/>[FR] SOLVATE MÉTHANOLIQUE DE SULFATE DE MORPHINE, SON PROCESSUS DE FABRICATION ET SES COMPOSITIONS ET PROCÉDÉS ASSOCIÉS DESTINÉS AU TRAITEMENT DE LA DOULEUR
  申请人：JOHNSON MATTHEY PLC

  公开号：WO2014140899A2

  公开（公告）日：2014-09-18

  Processes for reducing the amount of impurities, especially α,β-unsaturated ketones (ABUK), in materials containing morphine. Novel compounds, namely low ABUK morphine sulfate methanolic solvate, and a novel crystal form are also described. The method for making morphine sulfate methanolic solvate comprises mixing a morphine free base composition with methanol to form a solution and adding a liquid comprising sulfuric acid to the solution to form a morphine sulfate methanolic solvate precipitate. A method of making a morphine sulfate compound comprises drying the morphine sulfate methanolic solvate in the presence of water vapor, such that methanol molecules are removed and replaced with water vapor molecules. A composition for treating pain comprises the morphine sulfate compound and at least one pharmaceutically acceptable excipient. A method for treating pain comprises administering to a patient in need thereof the composition comprising the morphine sulfate compound and at least one pharmaceutically acceptable excipient.