双氟苯乙胺 | 50366-32-0

• 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: 双氟苯乙胺
• 中文别名: 氟苄胺
• 英文名称: 2-[bis(p-fluorophenyl)-methoxy]ethylamine
• 英文别名: 2-[Bis-(4-fluorphenyl)-methyloxy]ethylamin；Flunamine；2-[bis(4-fluorophenyl)methoxy]ethanamine
• CAS: 50366-32-0
• 化学式: C₁₅H₁₅F₂NO
• 分子量: 263.287
• InChiKey: BBEDRGWUDRUNQC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  19
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  35.2
• 氢给体数：
  1
• 氢受体数：
  4

安全信息

• 海关编码：
  2922199090

反应信息

• 作为反应物：
  描述：

  双氟苯乙胺 在 dimethyl sulfide borane 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 9.0h， 生成 [3-(4-Benzyl-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl)-propyl]-{2-[bis-(4-fluoro-phenyl)-methoxy]-ethyl}-amine
  参考文献：
  名称：

  New Substituted 1,4-Benzoxazine Derivatives with Potential Intracellular Calcium Activity

  摘要：

  Substituted 1,4-benzoxazines bearing an amino side chain at the 2-position were prepared and were found to have a moderate activity on intracellular calcium. Of the compounds studied it was found that those which possess a homoveratrylamino moiety exhibited superior potency. The chain length and the nature of the amine (4-fluorophenylpiperazine, 4-fluorobenzhydryloxyethylamine, N-substituted homoveratrylamine) is discussed. The 4-benzyl-3,4-dihydro-2[3-[[2-(3,4-dimethoxyphenyl)ethyl]amino]propyl]-2H-1,4-benzoxazine (3c) is the most potent derivative of the series with a ratio of IC50 values against PE (phenylephrine) and K+ of 2.1. Under these test conditions a ratio near 1 indicates potential intracellular calcium activity while a ratio greater than 100 an action on extracellular calcium influx.

  DOI：

  10.1021/jm970795t
• 作为产物：
  描述：

  2-[bis(4-fluorophenyl)methoxy]ethyl chloride 在 sodium hydroxide 、 氨 作用下， 以 甲醇 为溶剂， 生成 双氟苯乙胺
  参考文献：
  名称：

  Aminoalkylethers

  摘要：

  一般式为##STR1##的二苯甲氧基乙胺，其中R.sub.1代表氟、溴或氯原子，R.sub.2代表氢或氟原子，R.sub.3代表氢、氟或氯原子，但有以下限制条件：当R.sub.2为氟原子时，R.sub.3为氢原子；当R.sub.3为氯原子时，R.sub.1为氟原子；当R.sub.2和R.sub.3均为氢原子时，R.sub.1为氟或溴原子。还公开了它们的非毒性酸加盐。这些化合物具有多巴胺能特性，可用于治疗帕金森综合症。公开了用于此类用途的组合物。

  公开号：

  US04003932A1

文献信息

• Methods and compounds for treating depression and other disorders
  申请人：NPS PHARMACEUTICALS, INC.

  公开号：EP1790337A2

  公开（公告）日：2007-05-30

  The present invention features compounds active at both the serotonin reuptake site and the N-methyl-D-aspartate (NMDA) receptor and the use of such compounds for treating different disorders. Compounds having activity at the serotonin reuptake site and the NMDA receptor ("multi-active compounds") can be used to treat different types of disorders such as obsessive-compulsive disorders (OCD), sleep disorders, sexual dysfunction, and eating disorders.

  本发明的特点是具有在血清素再摄取位点和N-甲基-D-天门冬氨酸（NMDA）受体活性的化合物，并使用这些化合物治疗不同的疾病。具有在血清素再摄取位点和NMDA受体（“多功能化合物”）的活性的化合物可用于治疗不同类型的疾病，如强迫症障碍（OCD），睡眠障碍，性功能障碍和进食障碍。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• Aminoalkylethers; composition and method of use
  申请人：Gist-Brocades N.V.

  公开号：US04049825A1

  公开（公告）日：1977-09-20

  Diphenylmethoxyethylamines of the general formula ##STR1## in which R.sub.1 represents a fluorine, bromine or chlorine atom, R.sub.2 represents a hydrogen or fluorine atom and R.sub.3 represents a hydrogen, fluorine or chlorine atom, with the provisos that R.sub.3 is a hydrogen atom when R.sub.2 is a fluorine atom, R.sub.1 is a fluorine atom when R.sub.3 is a chlorine atom and R.sub.1 is a fluorine or bromine atom when R.sub.2 and R.sub.3 both are hydrogen atoms, and their non-toxic acid addition salts are disclosed. The compounds have dopaminergic properties and their use is indicated for treating the Parkinson syndrome. Compositions for such use are disclosed.

  本发明公开了一般式为##STR1##的二苯甲氧基乙胺类化合物，其中R.sub.1代表氟、溴或氯原子，R.sub.2代表氢或氟原子，R.sub.3代表氢、氟或氯原子，但须满足当R.sub.2为氟原子时，R.sub.3为氢原子；当R.sub.3为氯原子时，R.sub.1为氟原子；当R.sub.2和R.sub.3均为氢原子时，R.sub.1为氟或溴原子。此外，本发明还公开了这些化合物的无毒酸加盐，并且这些化合物具有多巴胺能作用，可用于治疗帕金森综合症。本发明还公开了用于此类用途的组合物。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。
• New prenylamine analogues: synthesis and Ca2+-entry blocking activity
  作者：PM Caldirola、H van der Goot、H Timmerman

  DOI：10.1016/0223-5234(92)90136-o

  日期：1992.9

  The synthesis of a series of diphenylalkylamine derivatives related to prenylamine is reported. The amphetamine group in the prenylamine structure was replaced by other moieties. In addition to substitutions in the aromatic rings, heteroatoms such as sulphur and oxygen were introduced in the chain. The calcium-entry blocking activity was assayed in binding experiments on a guinea-pig brain membrane preparation by displacing [H-3]-nitrendipine.