N-BOC-Β-甲基-4-溴苯乙胺 | 211314-91-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: N-BOC-Β-甲基-4-溴苯乙胺
• 英文名称: 1-[(1-tert-butoxycarbonylamino-1-methyl)ethyl]-4-bromobenzene
• 英文别名: 2-(4-bromophenyl)-N-(t-butoxycarbonyl)propylamine；[2-(4-bromo-phenyl)-propyl]-carbamic acid tert-butyl ester；Tert-butyl N-[2-(4-bromophenyl)propyl]carbamate
• CAS: 211314-91-9
• 化学式: C₁₄H₂₀BrNO₂
• 分子量: 314.222
• InChiKey: DWVQIDLQGUKRLS-UHFFFAOYSA-N

物化性质

• 沸点：
  397.9±25.0 °C(Predicted)
• 密度：
  1.254±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  18
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  38.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-BOC-Β-甲基-4-溴苯乙胺 在 四(三苯基膦)钯 potassium carbonate 、 三氟乙酸 作用下， 以 二氯甲烷 、 甲苯 为溶剂， 反应 20.0h， 生成 2-(2''-Fluoro-biphenyl-4-yl)-propylamine
  参考文献：
  名称：

  Biarylpropylsulfonamides as Novel, Potent Potentiators of 2-Amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic Acid (AMPA) Receptors

  摘要：

  DOI：

  10.1021/jm0002836
• 作为产物：
  描述：

  2-(4-溴苯基)丙腈 在 dimethyl sulfide borane 、 碳酸氢钠 作用下， 以 四氢呋喃 、 氯仿 为溶剂， 反应 1.0h， 生成 N-BOC-Β-甲基-4-溴苯乙胺
  参考文献：
  名称：

  Biarylpropylsulfonamides as Novel, Potent Potentiators of 2-Amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic Acid (AMPA) Receptors

  摘要：

  DOI：

  10.1021/jm0002836

文献信息

• Sulphonamide derivatives
  申请人：Eli Lilly and Company

  公开号：US06303816B1

  公开（公告）日：2001-10-16

  Glutamate receptor function in a mammal may be potentiated using an effective amount of a compound of formula R1—L—NHSO2R2  I in which R1 represents an unsubstituted or substituted aromatic or heteroaromatic group; R2 represents (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)fluoroalkyl, (1-6C)chloroalkyl, (2-6C)alkenyl, (1-4C)alkoxy(1-4C)alkyl, phenyl which is unsubstituted or substituted by halogen, (1-4C)alkyl or (1-4C)alkoxy, or a group, of formula R3R4N in which R3 and R4 each independently represents (1-4C)alkyl or, together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, morpholino, piperazinyl, hexahydroazepinyl or octahydroazocinyl group; and L represents a (2-4C)alkylene chain which is unsubstituted or substituted by one or two substituents selected independently from (1-6C)alkyl, aryl(1-6C)alkyl, (2-6C)alkenyl, aryl(2-6C)alkenyl and aryl, or by two substituents which, together with the carbon atom or carbon atoms to which they are attached form a (3-8C)carbocyclic ring; and pharmaceutically acceptable salts thereof. Also disclosed are compounds of formula I, processes for preparing them and pharmaceutical compositions containing them.

  在哺乳动物中，使用有效量的公式 I 所示化合物的谷氨酸受体功能可以被增强：R1—L—NHSO2R2  I 其中：R1 代表未取代或取代的芳香族或杂芳族基团；R2 代表 (1-6C) 烷基，(3-6C) 环烷基，(1-6C) 氟代烷基，(1-6C) 氯代烷基，(2-6C) 烯丙基，(1-4C) 烷氧基(1-4C) 烷基，未取代或被卤素、(1-4C) 烷基或(1-4C) 烷氧基取代的苯基，或者一个由 R3R4N 组成的基团，其中 R3 和 R4 各自独立地代表 (1-4C) 烷基，或者与它们所连接的氮原子一起形成一个氮杂环丁烷基、吡咯烷基、哌啶基、吗啡啉基、哌嗪基、六氢氮杂环庚基或八氢氮杂环辛基；L 代表一个未取代或取代有一个或两个独立选择的(1-6C) 烷基、芳基(1-6C) 烷基、(2-6C) 烯丙基、芳基(2-6C) 烯丙基和芳基的 (2-4C) 烷烯链，或者两个取代基，它们与它们所连接的碳原子或碳原子一起形成一个 (3-8C) 碳环烷基；以及它们的药物可接受的盐。还公开了公式 I 的化合物、它们的制备过程以及包含它们的药物组合物。
• Protective Agent for Retinal Neuronal Cell Comprising Indazole Derivative as Active Ingredient
  申请人：Seike Hisayuki

  公开号：US20090012123A1

  公开（公告）日：2009-01-08

  As a result of intensive studies for the purpose of finding a new medicinal use of an indazole derivative, it was found that an indazole derivative inhibits glutamate-induced retinal neuronal cell death in rat fetal retinal neuronal cells, in other words, the indazole derivative acts directly on the retinal neuronal cells and exhibits an effect of protecting retinal neuronal cells. Accordingly, the indazole derivative is useful for the prevention or treatment of an eye disease associated with retinal neuronal cell damage or retinal damage.

  经过对吲唑衍生物进行深入研究，目的是寻找其新的药用价值。研究发现，吲唑衍生物在大鼠胎儿视网膜神经细胞中能够抑制谷氨酸诱导的视网膜神经细胞死亡，换句话说，吲唑衍生物直接作用于视网膜神经细胞，并显示出保护视网膜神经细胞的效果。因此，吲唑衍生物对于预防或治疗与视网膜神经细胞损伤或视网膜损伤相关的眼病是有用的。
• [EN] NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES<br/>[FR] NOUVEAUX COMPOSÉS UTILES POUR LE TRAITEMENT DE MALADIES DÉGÉNÉRATIVES ET INFLAMMATOIRES
  申请人：GALAPAGOS NV

  公开号：WO2010010189A1

  公开（公告）日：2010-01-28

  Novel [1,2,4]triazolo[1,5-a]pyridine compounds are disclosed that have a Formula represented by the Formula (I). These compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotox in states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g. diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6 and transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.

  揭示了具有由公式（I）表示的公式的新型[1,2,4]三唑并[1,5-a]吡啶化合物。这些化合物可以制备为药物组合物，并可用于预防和治疗包括人类在内的哺乳动物的各种疾病，例如涉及软骨降解、骨骼和/或关节降解的疾病，例如骨关节炎；以及涉及炎症或免疫反应的疾病，如克罗恩病、类风湿性关节炎、牛皮癣、过敏性气道疾病（例如哮喘、鼻炎）、儿童特发性关节炎、结肠炎、炎性肠病、内毒素驱动的疾病状态（例如旁路手术后的并发症或慢性内毒素状态导致的慢性心力衰竭等），涉及软骨周转障碍的疾病（例如涉及软骨细胞合成刺激的疾病）、先天性软骨畸形、与IL6过度分泌和移植排斥（例如器官移植排斥）以及增生性疾病相关的疾病。
• [EN] TRYCYCLIC COMPOUNDS AND PBK INHIBITORS CONTAINING THE SAME<br/>[FR] COMPOSÉS TRICYCLIQUES ET INHIBITEURS DE PBK LES CONTENANT
  申请人：ONCOTHERAPY SCIENCE INC

  公开号：WO2011123419A1

  公开（公告）日：2011-10-06

  Trycyclic compounds are provided. These compounds are PBK inhibitors, and are useful for the treatment of PBK related diseases, including cancer.

  提供的是三环化合物。这些化合物是PBK抑制剂，可用于治疗与PBK相关的疾病，包括癌症。
• [EN] [1, 2, 4] TRIAZOLO [1, 5-A] PYRIDINES AS JAK INHIBITORS<br/>[FR] [1, 2, 4]TRIAZOLO[1, 5-A]PYRIDINES UTILISÉES COMME INHIBITEURS DE JAK
  申请人：GALAPAGOS NV

  公开号：WO2010010184A1

  公开（公告）日：2010-01-28

  Novel [1,2,4]triazolo[1,5-a]pyridine compounds are disclosed that have a Formula represented by the following: (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, joint disease, inflammation, and others.

  揭示了一种具有以下式表示的化学式的新型[1,2,4]三唑并[1,5-a]吡啶化合物（I）。这些化合物可以制备为药物组合物，并可用于预防和治疗包括人类在内的哺乳动物的各种疾病，例如关节疾病、炎症等。