2-bromo-4-cyclopentyloxy-3-hydroxybenzaldehyde

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-bromo-4-cyclopentyloxy-3-hydroxybenzaldehyde
• 英文别名: 2-bromo-4-cyclopentoxy-3-hydroxy-benzaldehyde
• 化学式: C₁₂H₁₃BrO₃
• 分子量: 285.137
• InChiKey: KEWMQGIFMNOGIJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  46.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-bromo-4-cyclopentyloxy-3-hydroxybenzaldehyde 在 palladium diacetate sodium tetrahydroborate 、 氯化亚砜 、 苄基三甲基氢氧化铵 、 sodium hydride 、 sodium carbonate 、 potassium carbonate 作用下， 以 四氢呋喃 、 乙二醇二甲醚 、 二氯甲烷 、 N,N-二甲基甲酰胺 、 乙腈 为溶剂， 反应 32.33h， 生成 5-cyano-5-(4-cyclopentyloxy-8-nitro-dibenzofuran-1-yl)-2-oxo-cyclohexane carboxylic acid methyl ester
  参考文献：
  名称：

  [EN] NOVEL HETEROCYCLIC COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESSES FOR THEIR PREPARATION
  [FR] NOUVEAUX COMPOSÉS HÉTÉROCYCLIQUES, COMPOSITIONS PHARMACEUTIQUES LES CONTENANT ET PROCÉDÉS POUR LEUR PRÉPARATION

  摘要：

  公开号：

  WO2009115874A3
• 作为产物：
  描述：

  4-cyclopentyloxy-3-hydroxybenzaldehyde 在 溴 、 sodium acetate 、 铁粉 作用下， 以 溶剂黄146 为溶剂， 以72%的产率得到2-bromo-4-cyclopentyloxy-3-hydroxybenzaldehyde
  参考文献：
  名称：

  多取代二苯并[ b，d ]呋喃的合成

  摘要：

  描述了由容易获得的起始原料合成多取代的二苯并[ b，d ]呋喃衍生物7a-b和11a-b。这些化合物是用于合成具有广泛治疗应用的分子的重要中间体。

  DOI：

  10.1002/jhet.5570450326

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。
• 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。
• 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.

  合成含有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-羧酰胺和其药学上可接受的盐的杂环化合物的方法。
• [EN] PROCESS FOR THE PREPARATION OF N-(3,5-DICHLOROPYRID-4-YL)-4DIFLUOROMETHOXY-8-METHANESULFONAMIDO-DIBENZO[B,D]FURAN-1-CARBOXAMIDE<br/>[FR] PROCEDE DE PREPARATION DE N-(3,5-DICHLOROPYRID-4-YL)-4-DIFLUOROMETHOXY-8-METHANESULFONAMIDO-DIBENZO[B,D]FURAN-1-CARBOXAMIDE
  申请人：GLENMARK PHARMACEUTICALS SA

  公开号：WO2006040652A2

  公开（公告）日：2006-04-20

  The present invention relates to a method of preparing N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-methanesulfonamido-dibenzo[b,d]furan-1-carboxamide and pharmaeutically acceptable salts thereof, such as its sodium salt, and novel intermediate compounds useful in the synthesis of the aforementioned compound.

  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。