来氟米特杂质G(EP)标准品 | 724429-16-7

• 物质功能分类: 分析化学 - 标准品 - 药典标准品和杂质标准品
• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 来氟米特杂质G(EP)标准品
• 中文别名: 来氟米特杂质G
• 英文名称: 5-methyl-isoxazole-4-carboxylic acid p-toluidide
• 英文别名: 5-Methyl-isoxazol-4-carbonsaeure-p-toluidid；5-methyl-N-(4-methylphenyl)-isoxazole-4-carboxamide；5-Methyl-N-(4-methylphenyl)isoxazole-4-carboxamide；5-methyl-N-(4-methylphenyl)-1,2-oxazole-4-carboxamide
• CAS: 724429-16-7
• 化学式: C₁₂H₁₂N₂O₂
• mdl: MFCD05156800
• 分子量: 216.239
• InChiKey: MIOYDAUCMWWNRH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.166
• 拓扑面积：
  55.1
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  来氟米特杂质G(EP)标准品 、 alkaline earth salt of/the/ methylsulfuric acid 生成 2-cyano-acetoacetic acid p-toluidide
  参考文献：
  名称：

  Dains; Griffin, Journal of the American Chemical Society, 1913, vol. 35, p. 969

  摘要：

  DOI：
• 作为产物：
  描述：

  2-acetyl-3-p-toluidino-acrylic acid p-toluidide 生成 来氟米特杂质G(EP)标准品
  参考文献：
  名称：

  Dains; Griffin, Journal of the American Chemical Society, 1913, vol. 35, p. 969

  摘要：

  DOI：

文献信息

• Method for systhesizing leflunomide
  申请人：——

  公开号：US20020022646A1

  公开（公告）日：2002-02-21

  A process for synthesizing leflunomide from 5-methylisoxazole-4-carboxylic acid and 4-trifluoromethylaniline is provided. Further provided is the leflunomide prepared by the inventive process, which is substantially free of difficult-to-separate impurities often found in leflunomide prepared by known methods, including N-(4-trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide, 5-methyl-N-(4-methylphenyl)-isoxazole-4-carboxamide and N-(4-trifluoromethylphenyl)-3-methyl-isoxazole-4-carboxamide. The invention further provides pharmaceutical compositions and dosage forms containing highly pure leflunomide and methods of treating disease using the leflunomide.

  提供一种从5-甲基异噁唑-4-羧酸和4-三氟甲基苯胺合成来氟米特的方法。进一步提供了通过创新方法制备的来氟米特，该方法基本上不含常见方法制备的来氟米特中难以分离的杂质，包括N-(4-三氟甲基苯基)-2-氰基-3-羟基丙烯酰胺、5-甲基-N-(4-甲基苯基)-异噁唑-4-羧酰胺和N-(4-三氟甲基苯基)-3-甲基异噁唑-4-羧酰胺。该发明还提供含有高纯度来氟米特的药物组合物和剂型，以及使用来氟米特治疗疾病的方法。
• [EN] A METHOD FOR SYNTHESIZING LEFLUNOMIDE<br/>[FR] PROCEDE PERMETTANT D'EFFECTUER LA SYNTHESE DU LEFLUNOMIDE
  申请人：TEVA PHARMA

  公开号：WO2001060363A1

  公开（公告）日：2001-08-23

  A process for synthesizing leflunomide from 5-methylisoxazole-4-carboxylic acid and 4-trifluoromethylaniline is provided. Further provided is the leflunomide prepared by the inventive process, which is substantially free of difficult-to-separate impurities often found in leflunomide prepared by known methods, including N-(4-trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide, 5-methyl-N-(4-methylphenyl)-isoxazole-4-carboxamide and N-(4-trifluoromethylphenyl)-3-methyl-isoxazole-4-carboxamide. The invention further provides pharmaceutical compositions and dosage forms containing highly pure leflunomide and methods of treating disease using the leflunomide.

  提供了一种从5-甲基异噁唑-4-羧酸和4-三氟甲基苯胺合成来氟米特的方法。此外，该创新方法制备的来氟米特基本上没有难以分离的杂质，这些杂质通常存在于已知方法制备的来氟米特中，包括N-(4-三氟甲基苯基)-2-氰基-3-羟基巴豆酰胺，5-甲基-N-(4-甲基苯基)-异噁唑-4-羧酰胺和N-(4-三氟甲基苯基)-3-甲基异噁唑-4-羧酰胺。该发明还提供了含有高纯度来氟米特的药物组合物和剂型，并提供了使用来氟米特治疗疾病的方法。
• Method for synthesizing leflunomide
  申请人：——

  公开号：US20040127532A1

  公开（公告）日：2004-07-01

  A process for synthesizing leflunomide from 5-methylisoxazole-4-carboxylic acid and 4-trifluoromethylaniline is provided. Further provided is the leflunomide prepared by the inventive process, which is substantially free of difficult-to-separate impurities often found in leflunomide prepared by known methods, including N-(4-trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide, 5-methyl-N-(4-methylphenyl)-isoxazole-4-carboxamide and N-(4-trifluoromethylphenyl)-3-methyl-isoxazole-4-carboxamide. The invention further provides pharmaceutical compositions and dosage forms containing highly pure leflunomide and methods of treating disease using the leflunomide.

  本发明提供一种从5-甲基异噁唑-4-羧酸和4-三氟甲基苯胺合成左氟氮酰胺的方法。本发明还提供了通过本发明方法制备的左氟氮酰胺，其基本上不含左氟氮酰胺已知方法中常见的难以分离的杂质，包括N-(4-三氟甲基苯基)-2-氰基-3-羟基巴豆酰胺，5-甲基-N-(4-甲基苯基)-异噁唑-4-羧酰胺和N-(4-三氟甲基苯基)-3-甲基异噁唑-4-羧酰胺。本发明还提供了含有高纯度左氟氮酰胺的药物组合物和剂型，以及使用左氟氮酰胺治疗疾病的方法。
• ANTI-CANCER PHOSPHONATE ANALOGS
  申请人：Boojamra Constantine G.

  公开号：US20100022467A1

  公开（公告）日：2010-01-28

  The invention is related to phosphorus substituted anti-cancer compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

  本发明涉及磷取代的抗癌化合物、含有这些化合物的组合物以及包括给予这些化合物的治疗方法，还涉及用于制备这些化合物的过程和中间体。
• Leflunomide of high purity
  申请人：TEVA PHARMACEUTICAL INDUSTRIES LTD.

  公开号：EP1473035A1

  公开（公告）日：2004-11-03

  Leflunomide prepared from 5-methylisoxazole-4-carboxylic acid and 4-trifluoromethylaniline is provided which is substantially free of difficult-to-separate impurities found in leflunomide prepared by known methods, including N-(4-trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide, 5-methyl-N-(4-methylphenyl)-isoxazole-4-carboxamide and N-(4-trifluoromethylphenyl)-3-methyl-isoxazole-4-carboxamide. The invention further provides pharmaceutical compositions and dosage forms containing highly pure leflunomide and methods of treating disease using the leflunomide.

  由 5-甲基异恶唑-4-羧酸和 4-三氟甲基苯胺制备的来氟米特基本上不含已知方法制备的来氟米特中难以分离的杂质、包括 N-(4-三氟甲基苯基)-2-氰基-3-羟基巴豆酰胺、5-甲基-N-(4-甲基苯基)-异恶唑-4-甲酰胺和 N-(4-三氟甲基苯基)-3-甲基-异恶唑-4-甲酰胺。本发明进一步提供了含有高纯度来氟米特的药物组合物和剂型，以及使用来氟米特治疗疾病的方法。