4-(二氟甲氧基)-8-硝基二苯并[b,d]呋喃-1-甲醛 | 685873-93-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并呋喃
• 中文名称: 4-(二氟甲氧基)-8-硝基二苯并[b,d]呋喃-1-甲醛
• 英文名称: 4-(difluoromethoxy)-8-nitrodibenzo[b,d]furan-1-carbaldehyde
• 英文别名: 4-difluoromethoxy-8-nitro-1-formyl dibenzo[b,d]furan；4-difluoromethoxy-8-nitro-1-formyl-dibenzo[b,d]furan；4-difluoromethoxy-8-nitro-1-formyldibenzo[b,d]furan；4-difluoromethoxy-8-nitro-1-formyl dibenzofuran；4-Difluoro methoxy-8-nitro-1-formyl dibenzo[b,d]furan；4-(difluoromethoxy)-8-nitrodibenzofuran-1-carbaldehyde
• CAS: 685873-93-2
• 化学式: C₁₄H₇F₂NO₅
• 分子量: 307.21
• InChiKey: OUOPTBPLTKNFSC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  22
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  85.3
• 氢给体数：
  0
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  4-(二氟甲氧基)-8-硝基二苯并[b,d]呋喃-1-甲醛 生成 4-(difluoromethoxy)-8-nitrodibenzo[b,d]furan-1-carboxylic acid
  参考文献：
  名称：

  [EN] PROCESS FOR THE PREPARATION OF N-(3,5-DICHLOROPYRID-4-YL)-4DIFLUOROMETHOXY-8-METHANESULFONAMIDO-DIBENZO[B,D]FURAN-1-CARBOXAMIDE
  [FR] PROCEDE DE PREPARATION DE N-(3,5-DICHLOROPYRID-4-YL)-4-DIFLUOROMETHOXY-8-METHANESULFONAMIDO-DIBENZO[B,D]FURAN-1-CARBOXAMIDE

  摘要：

  本发明涉及制备N-(3,5-二氯吡啶-4-基)-4-二氟甲氧基-8-甲磺酰基-二苯并[b,d]呋喃-1-羧酰胺及其药学上可接受的盐，如其钠盐，以及在合成上述化合物中有用的新的中间体化合物的方法。

  公开号：

  WO2006040652A2
• 作为产物：
  描述：

  氟里昂-22 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 4.0h， 以50%的产率得到4-(二氟甲氧基)-8-硝基二苯并[b,d]呋喃-1-甲醛
  参考文献：
  名称：

  [EN] PROCESS FOR THE PREPARATION OF N-(3,5-DICHLOROPYRID-4-YL)-4DIFLUOROMETHOXY-8-METHANESULFONAMIDO-DIBENZO[B,D]FURAN-1-CARBOXAMIDE
  [FR] PROCEDE DE PREPARATION DE N-(3,5-DICHLOROPYRID-4-YL)-4-DIFLUOROMETHOXY-8-METHANESULFONAMIDO-DIBENZO[B,D]FURAN-1-CARBOXAMIDE

  摘要：

  公开号：

  WO2006040652A3

文献信息

• [EN] NOVEL TRICYCLIC COMPOUNDS USEFUL FOR THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISORDERS: PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM<br/>[FR] NOUVEAUX COMPOSES TRICYCLIQUES UTILES POUR TRAITER LES TROUBLES INFLAMMATOIRES ET ALLERGIQUES, PROCEDE DE PREPARATION DE CES COMPOSES ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT
  申请人：GLENMARK PHARMACEUTICALS LTD

  公开号：WO2004037805A1

  公开（公告）日：2004-05-06

  The present invention relates to novel tricyclic compounds useful for the treatment of inflammatory conditions, diseases of the central nervous and insulin resistant diabetes.

  本发明涉及用于治疗炎症性疾病、中枢神经系统疾病和胰岛素抵抗性糖尿病的新型三环化合物。
• [EN] NOVEL HETEROCYCLIC COMPOUNDS USEFUL FOR THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISORDERS: PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM<br/>[FR] NOUVEAUX COMPOSES HETEROCYCLIQUES POUR LE TRAITEMENT DES AFFECTIONS INFLAMMATOIRES ET ALLERGIQUES, LEUR PROCEDE DE PREPARATION ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT
  申请人：GLENMARK PHARMACEUTICALS LTD

  公开号：WO2004089940A1

  公开（公告）日：2004-10-21

  The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the formula (1), their analogs, their tautomers, their enantiomers, their diasteromers, their regioisomers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxide, their pharmaceutically acceptable solvates and the pharmaceutical compositions containing them. The groups X, Ar, Y, P and R1-R4 are defined in claim 1.

  本发明涉及新颖的杂环化合物，它们的类似物，其互变异构体，其位置异构体，其立体异构体，其对映异构体，其二对映异构体，其多晶形式，其药用可接受盐，其适当的N-氧化物，其药用可接受溶剂和含有它们的药物组合物。本发明更具体地涉及公式（1）的新型磷酸二酯酶4型（PDE4）抑制剂，其类似物，其互变异构体，其对映异构体，其二对映异构体，其位置异构体，其立体异构体，其多晶形式，其药用可接受盐，其适当的N-氧化物，其药用可接受溶剂和含有它们的药物组合物。其中，X、Ar、Y、P 和 R1-R4 组在权利要求书中有定义。
• SYNTHESIS OF HETEROCYCLIC COMPOUNDS
  申请人：Araldi Gian-Luca

  公开号：US20080009632A1

  公开（公告）日：2008-01-10

  Methods for the synthesis of heterocyclic compounds including N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-methanesulfonamido-dibenzo[b,d]furan-1-carboxamide and pharmaceutically acceptable salts thereof.

  合成杂环化合物的方法，包括N-(3,5-二氯吡啶-4-基)-4-二氟甲氧基-8-甲磺酰氨基-二苯并[b,d]呋喃-1-羧酰胺及其药用盐。
• [EN] NOVEL PDE INHIBITORS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESSES FOR THEIR PREPARATION<br/>[FR] NOUVEAUX INHIBITEURS DE PHOSPHODIESTÉRASES, COMPOSITIONS PHARMACEUTIQUES LES CONTENANT ET LEURS PROCÉDÉS DE PRÉPARATION
  申请人：MATRIX LAB LTD

  公开号：WO2009147476A1

  公开（公告）日：2009-12-10

  The present invention relates to novel heterocyclic compounds of general formula (I), which are phosphodiesterase inhibitors (PDEs), in particular phosphodiesterase type 4 inhibitors, pharmaceutical compositions containing them, and processes for their preparation. These novel PDEs are useful in treating allergic and inflammatory diseases (such as asthma, COPD, allergic rhinitis, allergic conjunctivitis, respiratory distress syndrome, chronic bronchitis, nephritis, rheumatoid spondylitis, osteoarthritis, atopic dermatitis, eosinophilic granuloma, psoriasis, rheumatoid septic shock, ulcerative colitis, multiple sclerosis, chronic inflammation, Crohn's syndrome and central nervous system(CNS) disorders) and for inhibiting the production of Tumor Necrosis Factor(TNF-α).

  本发明涉及一种新型杂环化合物，其一般式为(I)，它们是磷酸二酯酶抑制剂（PDEs），特别是磷酸二酯酶4型抑制剂，包含它们的制药组合物以及它们的制备方法。这些新型PDEs在治疗过敏和炎症性疾病（如哮喘、慢性阻塞性肺病、过敏性鼻炎、过敏性结膜炎、呼吸窘迫综合征、慢性支气管炎、肾炎、类风湿脊柱炎、骨关节炎、特应性皮炎、嗜酸性肉芽肿、银屑病、类风湿败血症、溃疡性结肠炎、多发性硬化症、慢性炎症、克罗恩综合征和中枢神经系统（CNS）疾病）以及抑制肿瘤坏死因子（TNF-α）的产生方面具有用途。
• Heterocyclic compounds useful for the treatment of inflammatory and allergic disorders
  申请人：Glenmark Pharmaceuticals, S.A.

  公开号：US07393846B2

  公开（公告）日：2008-07-01

  The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the Formula (1), their analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxide, pharmaceutically acceptable solvates and the pharmaceutical compositions containing them.

  本发明涉及新型杂环化合物及其类似物、互变异构体、位置异构体、立体异构体、对映异构体、二对映异构体、多晶型、药学上可接受的盐、适当的N-氧化物、药学上可接受的溶剂化物和含有它们的制药组合物。本发明更具体地涉及公式（1）的新型磷酸二酯酶4（PDE4）抑制剂及其类似物、互变异构体、对映异构体、二对映异构体、位置异构体、立体异构体、多晶型、药学上可接受的盐、适当的N-氧化物、药学上可接受的溶剂化物和含有它们的制药组合物。