2-(2-amino-5-fluorophenyl)ethanol | 553661-24-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-(2-amino-5-fluorophenyl)ethanol
• CAS: 553661-24-8
• 化学式: C₈H₁₀FNO
• 分子量: 155.172
• InChiKey: HOCPHZKDNNMZTQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  46.2
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-(2-amino-5-fluorophenyl)ethanol 、 三氟乙酸 在 四氯化碳 、 三乙胺 、 三苯基膦 作用下， 以89%的产率得到2,2,2-trifluoro-1-(5-fluoroindolin-1-yl)ethan-1-one
  参考文献：
  名称：

  One-Pot Cyclization of 2-Aminophenethyl Alcohols:  A Novel and Direct Approach to the Synthesis of N-Acyl Indolines

  摘要：

  [Graphics]A unique one-pot cyclization of 2-aminophenethyl alcohols with carboxylic acids in the presence of PPh3, CCl4, and NEt3 furnished the formation of N-acyl indolines in good to excellent yields. This new approach provides an efficient, scalable, low-cost, and direct access to the biologically important indolines which are further oxidizable to indoles and oxindoles.

  DOI：

  10.1021/jo701566v

文献信息

• Urea derivatives
  申请人：Yura Takeshi

  公开号：US20050154230A1

  公开（公告）日：2005-07-14

  This invention relates to urea derivatives and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The urea derivatives of the present invention has an excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, incontinence and/or inflammatory disorders.

  这项发明涉及脲衍生物及其盐，可用作制药制剂的活性成分。本发明的脲衍生物具有出色的VR1拮抗剂活性，可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗急迫性尿失禁、过度活动膀胱、慢性疼痛、神经痛、术后疼痛、类风湿关节痛、神经痛、神经病、疼痛、神经损伤、缺血、神经退行性疾病、中风、失禁和/或炎症性疾病的治疗。
• Process for producing indoles
  申请人：RESEARCH ASSOCIATION FOR UTILIZATION OF LIGHT OIL

  公开号：EP0182256B1

  公开（公告）日：1992-10-07
• UREA DERIVATIVES AS VR1-ANTAGONISTS
  申请人：Bayer HealthCare AG

  公开号：EP1461311A2

  公开（公告）日：2004-09-29
• US4757152A
  申请人：——

  公开号：US4757152A

  公开（公告）日：1988-07-12
• [EN] UREA DERIVATIVES AS VR1- ANTAGONISTS<br/>[FR] DERIVES D'UREE
  申请人：BAYER AG

  公开号：WO2003055848A2

  公开（公告）日：2003-07-10

  This invention relates to urea derivatives of the formula (I), its tautomeric or stereoisomeric form, or a salt thereof: (I) wherein Y is R1- R6 and X have the same meanings given in the description, which is useful as an active ingredient of pharmaceutical preparations. The urea derivatives of the present invention has an excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, incontinence and/or inflammatory disorders.