N-[1-R-2-(4-Methylphenyl)-1-methylethyl]-2-R-2-hydroxy-2-phenyl ethanamine | 81601-74-3

• 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: N-[1-R-2-(4-Methylphenyl)-1-methylethyl]-2-R-2-hydroxy-2-phenyl ethanamine
• 英文别名: (1R)-2-[[(2R)-1-(4-methylphenyl)propan-2-yl]amino]-1-phenylethanol
• CAS: 81601-74-3
• 化学式: C₁₈H₂₃NO
• 分子量: 269.387
• InChiKey: UHJAKRAAKOTZGB-QAPCUYQASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  20
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  32.3
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• Processes for producing optically active 2-amino-1-phenylethanol derivatives
  申请人：Daicel Chemical Industries, Ltd.

  公开号：US20030143701A1

  公开（公告）日：2003-07-31

  An (R)-2-amino-1-phenylethanol derivative shown by the general formula (IIa) 1 wherein R 1 and R 5 represent a hydrogen atom, etc.; R 2 , R 3 and R 4 independently represent a halogen atom, etc., or a salt thereof, can readily be produced (1) by permitting a microorganism belonging to the genus Rhodosporidium, the genus Comamonas or the like to act on a mixture of corresponding (R)-form and (S)-form to asymmetrically utilize, or (2) by permitting a microorganism belonging to the genus Lodderomyces, the genus Pilimelia or the like to act on a corresponding aminoketone derivative to asymmetrically reduce. An (R,R)-1-phenyl-2-[(2-phenyl-1-alkylethyl)amino]ethanol derivative having a high optical purity can easily be obtained from the compound of the formula (IIa) or a salt thereof. Said derivative is useful as an intermediate for producing an anti-obesity agent and so on.

  通式（IIa）所示的（R）-2-氨基-1-苯乙醇衍生物，其中R1和R5代表氢原子等；R2、R3和R4分别独立地表示卤素原子等，或其盐，可以通过（1）让属于红孢霉属、普通小杆菌属或类似菌属的微生物作用于相应（R）-型和（S）-型的混合物以不对称利用，或（2）让属于洛德罗霉属、皮利米利亚属或类似菌属的微生物作用于相应的氨基酮衍生物以不对称还原而轻松制备。可以从式（IIa）化合物或其盐中轻松获得具有高光学纯度的（R，R）-1-苯基-2-［（2-苯基-1-烷基乙基）氨基］乙醇衍生物。所述衍生物可用作生产抗肥胖剂等中间体。
• Compositions comprising a beta-antagonist and a beta-agonist, their preparation, and their use in treating obese humans and animals
  申请人：BEECHAM GROUP PLC

  公开号：EP0085514A2

  公开（公告）日：1983-08-10

  A pharmaceutieally acceptable composition comprising a β-agonist and a β-antagonist selected from propranolol, sotalol, atenolol, metoprolot, and salts or esters thereof, useful in the treatment of obese humans or animals. The composition is particularly useful in the treatment of an obese human, or animal suffering from a heart complaint. In which case the treatment with a β-agonist alone may unacceptably aggravate the heart complaint.

  一种药学上可接受的组合物，包含一种β-受体激动剂和一种选自普萘洛尔、索他洛尔、阿替洛尔、美托洛尔及其盐或酯类的β-受体激动剂，可用于治疗肥胖的人或动物。该组合物尤其适用于治疗肥胖的人或患有心脏疾病的动物。在这种情况下，单独使用β-受体激动剂可能会使心脏疾病恶化到不可接受的程度。
• Arylethanolamine derivatives, their preparation and use in pharmaceutical compositions
  申请人：BEECHAM GROUP PLC

  公开号：EP0040000B1

  公开（公告）日：1983-10-12
• US4588749A
  申请人：——

  公开号：US4588749A

  公开（公告）日：1986-05-13
• US5629200A
  申请人：——

  公开号：US5629200A

  公开（公告）日：1997-05-13