N-[2-(9H-carbazol-2-yloxy)ethyl]amine | 193761-39-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: N-[2-(9H-carbazol-2-yloxy)ethyl]amine
• 英文别名: 2-(9H-carbazol-2-yloxy)ethylamine；2-(9H-carbazol-2-yloxy)ethanamine
• CAS: 193761-39-6
• 化学式: C₁₄H₁₄N₂O
• 分子量: 226.278
• InChiKey: FUJRUPJWQSMMPG-UHFFFAOYSA-N

物化性质

• 沸点：
  459.5±25.0 °C(Predicted)
• 密度：
  1?+-.0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  51
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-[2-(9H-carbazol-2-yloxy)ethyl]amine 在 苯甲醛 作用下， 以 甲醇 、 氩 为溶剂， 生成 N-benzyl-N-[2-(9H-carbazol-2-yloxy)ethyl]amine
  参考文献：
  名称：

  PROCESS FOR THE PREPARATION OF TRICYCLIC AMINO ALCOHOL DERIVATIVES

  摘要：

  一种用于制备式（1）的三环氨基醇衍生物或其盐的方法，该方法有助于治疗和预防糖尿病、肥胖、高脂血症等疾病；以及用于该方法的中间体：其中R1是较低的烷基或苄基；*1代表一个不对称碳原子；R2是氢、卤素或羟基；A是以下组之一：（其中X是NH、O或S；R6是氢、羟基、氨基或乙酰氨基；当R6不是氢时，*2代表一个不对称碳原子）

  公开号：

  EP1195371A1

文献信息

• Process for preparing optically active secondary alcohols having nitrogenous or oxygenic functional groups
  申请人：——

  公开号：US20030045727A1

  公开（公告）日：2003-03-06

  A process for preparing optically active secondary alcohols of the general formula (3), [wherein R 1 is linear lower alkyl, an aromatic ring group, or the like; A is CH 2 NR 2 R 3 or the like; n is an integer of 0 to 2; and * represents an asymmetric carbon atom] by asymmetrically hydrogenating a ketone compound of the general formula (1) having nitrogenous or oxygen functional group at any of the a-, &bgr;- and &ggr;-positions, with selectivity among functional groups by the use of a ruthenium/optically active bidentate phosphine/diamine complex as the catalyst in the presence of hydrogen alone or together with a base. The optically active secondary alcohols obtained by the process are useful as drugs and intermediates for the preparation of drugs.

  通过使用钌/光学活性双齿膦/二胺配合物作为催化剂，在存在氢气的情况下或与碱一起，通过不对称地氢化具有氮或氧官能团在α、β和γ位置中的酮化合物（1）来制备通式（3）的光学活性二级醇，[其中R1是线性低碳烷基、芳香环基等；A是CH2NR2R3或类似物；n是0到2的整数；*代表不对称碳原子]。通过该过程获得的光学活性二级醇可用作药物及药物中间体的制备。
• Novel tricyclic compounds and drug compositions containing same
  申请人：ASAHI KASEI KOGYO KABUSHIKI KAISHA

  公开号：US20030139475A1

  公开（公告）日：2003-07-24

  Compounds having a &bgr;-3 adrenaline receptor agonist and are useful as drugs for the treatment and prevention of diabetes, obesity, hyperlipemia, etc., represented by a general formula (I) and salts thereof, and a process for producing these, and their intermediates, wherein R represents hydrogen or methyl; R 1 represents hydrogen, halogen, hydroxy, benzyloxy, amino, or hydroxymethyl; R 2 represents hydrogen, hydroxymethyl, NHR 3 , SO 2 NR 4 R 4′ , or nitro; R 6 represents hydrogen or lower alkyl; and X represents nitrogen, R 9 represents hydrogen, one of R 7 and R 8 represent hydrogen, and the other thereof represents hydrogen, amino, acetylamino, or hydroxy.

  具有&bgr;-3肾上腺素受体激动剂的化合物，可用于治疗和预防糖尿病、肥胖症、高脂血症等疾病，其通式表示为(I)，并且包括其盐，以及制备这些化合物和其中间体的方法。其中，R代表氢或甲基；R1代表氢、卤素、羟基、苄氧基、氨基或羟甲基；R2代表氢、羟甲基、NHR3、SO2NR4R4′或硝基；R6代表氢或低碳基；X代表氮；R9代表氢；R7和R8中的一个代表氢，而另一个代表氢、氨基、乙酰氨基或羟基。
• Method for manufacturing tricyclic amino alcohol derivatives
  申请人：Asahi Kasei Kabushiki Kaisha

  公开号：US06495701B1

  公开（公告）日：2002-12-17

  The present invention is directed to processes for the preparation of a compound useful for treating diabetes, obesity, hyperlipidemia and the like, which compound is represented by the formula (1): wherein R1 represents a lower alkyl group or a benzyl group; *1 represents an asymmetric carbon atom; R2 hydrogen atom, a halogen atom or a hydroxyl group; and A represents one of the following groups: wherein X represents NH, O or S; R6 represents a hydrogen atom, a hydroxyl group, an amino group or an acetylamino group; and *2 represents an asymmetric carbon atom when R6 is not a hydrogen atom, and to intermediates useful for the said processes. The processes of the present invention are convenient, practical preparing processes with low cost which comprise a small number of steps with good industrial work efficiency.

  本发明涉及一种用于治疗糖尿病、肥胖症、高脂血症等疾病的化合物的制备方法，该化合物由公式（1）表示：其中，R1代表较低的烷基或苄基；*1代表不对称碳原子；R2代表氢原子、卤素原子或羟基；A代表以下一种基团之一：其中，X代表NH、O或S；R6代表氢原子、羟基、氨基或乙酰氨基；当R6不是氢原子时，*2代表不对称碳原子，并且本发明还涉及用于上述方法的中间体。本发明的方法是方便实用的制备方法，成本低廉，步骤少，工业效率高。
• NOVEL TRICYCLIC COMPOUNDS AND DRUG COMPOSITIONS CONTAINING THE SAME
  申请人：Asahi Kasei Kogyo Kabushiki Kaisha

  公开号：EP0882707A1

  公开（公告）日：1998-12-09

  Compounds represented by general formula (I) or salts thereof, a process for producing the same, and intermediates therefor, wherein R represents hydrogen or methyl; R1 represents hydrogen, hologeno, hydroxy, benzyloxy, amino, or hydroxymethyl; R2 represents hydrogen, hydroxymethyl, NHR3, SO2NR4R4, or nitro; R6 represents hydrogen or lower alkyl; and X represents nitrogen, oxygen, sulfur, or methylene, provided that when X represents nitrogen, oxygen, or sulfur, then R9 represents hydrogen, one of R7 an R8 represents hydrogen, and the other thereof represents hydrogen, amino, acetylamino, or hydroxy, and when X represents methylene, then R7 and R8 each represents hydrogen and R9 represents hydrogen, amino, etc. They have a β-3 adrenaline receptor agonist and are useful as drugs for the treatment and prevention of diabetes, obesity, hyperlipemia, etc.

  通式(I)所代表的化合物或其盐类，以及生产该化合物或其盐类的工艺和中间体，其中R代表氢或甲基；R1代表氢、囟素、羟基、苄氧基、氨基或羟甲基；R2代表氢、羟甲基、NHR3、SO2NR4R4或硝基；R6代表氢或低级烷基；X代表氮、氧、硫或亚甲基，但当X代表氮、氧或硫时，R9代表氢，R7和R8中的一个代表氢，另一个代表氢、氨基、乙酰氨基或羟基；当X代表亚甲基时，R7和R8各自代表氢，R9代表氢、氨基等。它们具有β-3肾上腺素受体激动剂的作用，可作为治疗和预防糖尿病、肥胖症、高脂血症等的药物。
• NOVEL METHOD FOR MANUFACTURING TRICYCLIC AMINO ALCOHOL DERIVATIVES
  申请人：Asahi Kasei Kabushiki Kaisha

  公开号：EP1174425A1

  公开（公告）日：2002-01-23

  The present invention is directed to processes for the preparation of a compound useful for treating and preventing diabetes, obesity, hyperlipidemia and the like, which compound is represented by the formula (1) : wherein R1 represents a lower alkyl group or a benzyl group; ∗1 represents an asymmetric carbon atom; R2 represents a hydrogen atom, a halogen atom or a hydroxyl group; and A represents one of the following groups: wherein X represents NH, O or S; R6 represents a hydrogen atom, a hydroxyl group, an amino group or an acetylamino group; and ∗2 represents an asymmetric carbon atom when R6 is not a hydrogen atom, and to intermediates useful for the said processes. The processes of the present invention are convenient, practical preparing processes with low cost which comprise a small number of steps with good industrial work efficiency.

  本发明涉及一种用于治疗和预防糖尿病、肥胖症、高脂血症等的化合物的制备工艺，该化合物由式(1)表示： 其中 R1 代表低级烷基或苄基；∗1 代表不对称碳原子；R2 代表氢原子、卤素原子或羟基；A 代表下列基团之一： 其中 X 代表 NH、O 或 S；R6 代表氢原子、羟基、氨基或乙酰氨基；当 R6 不是氢原子时，∗2 代表不对称碳原子。本发明的工艺是方便实用的制备工艺，成本低，步骤少，工业生产效率高。