3-formyl-2,3,4,5-tetrahydro-1H-3-benzazepine | 215033-43-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 英文名称: 3-formyl-2,3,4,5-tetrahydro-1H-3-benzazepine
• 英文别名: 1,2,4,5-tetrahydro-3H-3-benzazepine-3-carboaldehyde；1,2,4,5-tetrahydro-3-benzazepine-3-carbaldehyde
• CAS: 215033-43-5
• 化学式: C₁₁H₁₃NO
• 分子量: 175.23
• InChiKey: VAJSDEJKCNNELG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  3-formyl-2,3,4,5-tetrahydro-1H-3-benzazepine 在 sodium hydroxide 作用下， 以 乙醇 为溶剂， 反应 1.0h， 以77%的产率得到2,3,4,5 -四氢-1H -苯并[D]氮杂卓
  参考文献：
  名称：

  A Synthesis of 2,3,4,5-Tetrahydro-1H-3-benzazepines via Pummerer-Type Cyclization of N-(2-Arylethyl)-N-(2-phenylsulfinylethyl)formamides

  摘要：

  DOI：

  10.3987/com-00-8982
• 作为产物：
  描述：

  N-[2-(2-bromophenyl)ethyl]-N-(2-(phenylthio)ethyl)formamide 在 三正丁基氢锡 、 碳酸氢钠 、 间氯过氧苯甲酸 、 1,1'-偶氮(氰基环己烷) 作用下， 以 二氯甲烷 、 甲苯 、 xylene 为溶剂， 反应 15.0h， 生成 3-formyl-2,3,4,5-tetrahydro-1H-3-benzazepine
  参考文献：
  名称：

  7-endo Selective Aryl Radical Cyclization onto Enamides Leading to 3-Benzazepines:  Concise Construction of a Cephalotaxine Skeleton

  摘要：

  Bu3SnH-mediated radical cyclizations of 2-(2-bromophenyl)N-ethenylacetamide gave 6-exo cyclization product 15 as the major product, whereas N-[2-(2-bromophenyl)ethyl]-N-ethenylamides gave almost exclusively 7-endo cyclization products. These results indicated that the position of the carbonyl group on enamide played an important role in deciding the course of the cyclization. The 7-endo selective cyclization was applied to concise construction of a cephalotaxine skeleton.

  DOI：

  10.1021/jo040264u

文献信息

• Thermogenic composition and benzazepine thermogenics
  申请人：Takeda Chemical Industries, Inc.

  公开号：US06534496B1

  公开（公告）日：2003-03-18

  The object of the present invention is to provide a prophylactic and/or therapeutic drug for obesity and obesity-associated diseasestor diabetes with a reduced risk for central side effects and high universality in usage. Another object of the present invention is to provide a pharmaceutical composition comprising a compound of the following formula: wherein Ar represents phenyl which may be substituted and/or condensed; n represents an integer of 1 to 10; R represents hydrogen or a hydrocarbon group which may be substituted, which may not be the same in its n occurrences; R may be bound to either Ar or a substituent for Ar; Y represents an amino group which may be subsituted or a nitrogen-containing saturated heterocyclic group which may be substituted, or a salt thereof, which can be used for a thermogenic agent, an antiobesity agent, a lipolytic agent, or a prophylactic and/or treating drug for obesity-associated diseases.

  本发明的目的是提供一种用于肥胖和肥胖相关疾病或糖尿病的预防和/或治疗药物，其具有降低中枢副作用风险和高普遍性的特点。本发明的另一个目的是提供一种包含以下式的化合物的药物组合物： 其中Ar代表可能被取代和/或缩合的苯基；n代表1到10的整数；R代表氢或可能被取代的碳氢基团，在其n次出现时可能不相同；R可以与Ar或Ar的取代物结合；Y代表可能被取代的氨基或可能被取代的含氮饱和杂环基团，或其盐，可用作热原药剂、抗肥胖药剂、脂肪分解药剂，或肥胖相关疾病的预防和/或治疗药物。
• Preventives and remedies for central nervous system diseases
  申请人：——

  公开号：US20030207863A1

  公开（公告）日：2003-11-06

  A prophylactic or therapeutic agent for central nervous system diseases based on amyloid &bgr;40 secretion inhibitory activity of a compound having urotensin II receptor antagonistic activity or a salt thereof.

  一种预防或治疗中枢神经系统疾病的药剂，基于一种具有尿泰松II受体拮抗活性或其盐的化合物对淀粉样蛋白β40分泌抑制活性。
• Uses of polypeptides
  申请人：——

  公开号：US20040053826A1

  公开（公告）日：2004-03-18

  The present invention provides uses of a polypeptide having a ligand activity to a sensory epithelium neuropeptide-like receptor (SENR) which is a G protein-coupled receptor protein, and a DNA encoding the same. More specifically, the present invention provides an anti-attention-deficit-disorder or anti-narcolepsy agent, which comprises a polypeptide having a ligand activity for SENR or a salt thereof, as well as a method for screening compounds having an anti-attention-deficit-disorder or anti-narcolepsy activity or compounds having an anti-anxiety, anti-depression, anti-insomnia, anti-schizophrenia or anti-fear activity or salts thereof, which comprises using the above polypeptide or a precursor protein of the polypeptide or a salt thereof.

  本发明提供了一种具有配体活性的多肽对感觉上皮神经肽样受体（SENR）的用途，该受体是一种G蛋白偶联受体蛋白，以及编码该多肽的DNA。更具体地，本发明提供了一种抗注意缺陷失调或抗嗜睡症药剂，它包括具有SENR配体活性或其盐的多肽，以及一种筛选具有抗注意缺陷失调或抗嗜睡症活性或具有抗焦虑、抗抑郁、抗失眠、抗精神分裂症或抗恐惧活性或其盐的化合物的方法，该方法包括使用上述多肽或其前体蛋白或其盐。
• Gpr14 antagonist
  申请人：——

  公开号：US20040063699A1

  公开（公告）日：2004-04-01

  A novel GPR14 antagonist. The GPR14 antagonist comprises a compound represented by the formula (I) or a salt thereof wherein Ar represents optionally substituted aryl; X represents a spacer; n is an integer of 1 to 10; R represents an optionally substituted hydrocarbon group, etc., provided that R may be bonded to Ar, etc. to form a ring; and Y represents optionally substituted amino, etc. 1

  一种新型的GPR14拮抗剂。该GPR14拮抗剂包括由式(I)或其盐所表示的化合物，其中Ar代表可选取代的芳基; X代表一个间隔物; n为1到10的整数; R代表可选取代的碳氢基团等，但R可以与Ar等连接形成环; Y代表可选取代的氨基等。
• 1,1'-Diadamantyl carboxylic acids, medicaments containing such compounds and their use
  申请人：Eckhardt Matthias

  公开号：US20110269736A1

  公开（公告）日：2011-11-03

  The present invention relates to compounds defined by formula (I) wherein the group R is defined as in claim 1 , possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases.

  本发明涉及具有有价值的药理活性的公式（I）所定义的化合物，其中R基团如权利要求1所定义。特别地，这些化合物是11β-羟基类固醇脱氢酶（HSD）1的抑制剂，因此适用于治疗和预防可以通过抑制该酶而受到影响的疾病，例如代谢性疾病。