1-amino-4-[5-(morpholin-4-ylmethyl)fur-2-yl]naphthalene | 294851-93-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 1-amino-4-[5-(morpholin-4-ylmethyl)fur-2-yl]naphthalene
• 英文别名: 4-[5-(morpholin-4-ylmethyl)furan-2-yl]naphthalen-1-amine
• CAS: 294851-93-7
• 化学式: C₁₉H₂₀N₂O₂
• 分子量: 308.38
• InChiKey: IJLMFMVGZPXOAN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  51.6
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-amino-4-[5-(morpholin-4-ylmethyl)fur-2-yl]naphthalene 、 2,2,2-三氯乙基 3-叔丁基-1-(4-甲基苯基)-1H-吡唑-5-基氨基甲酸酯 在 N,N-二异丙基乙胺 作用下， 以 二甲基亚砜 、 乙酸乙酯 、 乙腈 为溶剂， 生成 1-[3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl]-3-{4-[5-(morpholin-4-ylmethyl)fur-2-yl]naphthalen-1-yl} urea
  参考文献：
  名称：

  Polymorph and process for preparing same

  摘要：

  本文披露了用于制备式(I)的芳基和杂芳基取代脲化合物的过程、多形态和中间化合物，其中Ar1、Ar2、L、Q和X如本文所述。所得化合物在制备药物组合物中有用，用于治疗涉及炎症的疾病或病理条件，如慢性炎症性疾病。

  公开号：

  US20030109703A1
• 作为产物：
  描述：

  5-溴-2-呋喃甲醛 在 三丁基氯化锡 、 叔丁基锂 、 三乙酰氧基硼氢化钠 、 溶剂黄146 作用下， 以 四氢呋喃 为溶剂， 反应 27.0h， 生成 1-amino-4-[5-(morpholin-4-ylmethyl)fur-2-yl]naphthalene
  参考文献：
  名称：

  New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site

  摘要：

  Discovery of the pyrazole-naphthyl urea class of p38 MAP kinase inhibitors typified by the clinical candidate BIRB 796 has encouraged further exploration of this particular scaffold. Modification to the part of the inhibitor that occupies the adenine/ ATP binding site has resulted in a new way to obtain potent inhibitors that possess favorable in vitro and in vivo properties. (c) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.05.042

文献信息

• Novel carbamate and oxamide compounds
  申请人：Boehringer Ingelheim Pharmaceuticals, Inc.

  公开号：US20030092702A1

  公开（公告）日：2003-05-15

  Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or conditions such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds. 1

  本文披露了一种新型芳香化合物，其化学式为(I)，其中G、E、W、Ar、X、Y和Z如本文所述。这些化合物可用于治疗细胞因子介导的疾病或病况，如慢性炎症性疾病。还披露了含有这些化合物的药物组合物和制备这些化合物的方法。
• Process for synthesis of heteroaryl-substituted urea compounds useful as antiinflammatory agents
  申请人：Boehringer Ingelheim Pharmaceuticals, Inc.

  公开号：US20030181718A1

  公开（公告）日：2003-09-25

  Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar 1 , Ar 2 , L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. 1

  本发明涉及制备式(I)中的芳基和杂芳基取代的脲化合物的新工艺和新中间体化合物，其中Ar1，Ar2，L，Q和X如本文所述。所得的化合物可用于制备药物组合物，用于治疗涉及炎症的疾病或病理条件，如慢性炎症性疾病。
• Intermediates useful for synthesis of heteroaryl-substituted urea compounds, and processes of making same
  申请人：Zhang Lin-Hua

  公开号：US06894173B2

  公开（公告）日：2005-05-17

  Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar 1 , Ar 2 , L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.

  本发明涉及制备式(I)的芳基和杂芳基取代脲类化合物的新工艺和新中间体化合物，其中Ar1、Ar2、L、Q和X在此被描述。所得化合物可用于制备药物组合物，用于治疗涉及炎症的疾病或病理条件，如慢性炎症性疾病。
• PROCESS FOR SYNTHESIS OF HETEROARYL-SUBSTITUTED UREA COMPOUNDS
  申请人：Boehringer Ingelheim Pharmaceuticals Inc.

  公开号：EP1200411B1

  公开（公告）日：2005-12-14
• NOVEL PROCESS FOR SYNTHESIS OF HETEROARYL-SUBSTITUTED UREA COMPOUNDS
  申请人：BOEHRINGER INGELHEIM PHARMACEUTICALS INC.

  公开号：EP1200411A2

  公开（公告）日：2002-05-02