phenyl(4-(trifluoromethyl)phenyl)methanamine

• 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: phenyl(4-(trifluoromethyl)phenyl)methanamine
• 英文别名: 4-Trifluormethyl-benzhydrylamin；4-Trifluormethylbenzhydrylamin；phenyl-[4-(trifluoromethyl)phenyl]methanamine
• 化学式: C₁₄H₁₂F₃N
• mdl: MFCD04037376
• 分子量: 251.251
• InChiKey: AKMMVPFDNDRZLO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.142
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  phenyl(4-(trifluoromethyl)phenyl)methanamine 在 2,4,6-triphenylpyrylium tetrafluoroborate 作用下， 以 二氯甲烷 为溶剂， 反应 10.17h， 生成 4-(三氟甲基)二苯甲酮
  参考文献：
  名称：

  氢键通过光氧化还原催化胺的需氧氧化†

  摘要：

  据报道，在有机光催化剂的催化下，H键相互作用可指导胺的α-C–H氧化为酰胺和氨基酮。带有脲基团的吡咯烷，二芳基胺和苄基胺的好氧氧化具有高收率和广泛的底物范围，证明了该方法的高效率。

  DOI：

  10.1039/c8cc06603e
• 作为产物：
  描述：

  4-(三氟甲基)二苯甲酮 在 palladium on activated charcoal 吡啶 、 氨 、 氢气 作用下， 以 甲醇 为溶剂， 反应 16.0h， 生成 phenyl(4-(trifluoromethyl)phenyl)methanamine
  参考文献：
  名称：

  α-Methylation at benzylic fragment of N-aryl-N′-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model

  摘要：

  SAR studies for N-aryl-N '-benzyl urea class of TRPV1 antagonists have been extended to cover alpha-benzyl alkylation. Alkylated compounds showed weaker in vitro potencies in blocking capsaicin activation of TRPV1 receptor, but possessed improved pharmacokinetic properties. Further structural manipulations that included replacement of isoquinoline core with indazole and isolation of single enantiomer led to TRPV1 antagonists like (R)-16a with superior pharmacokinetic properties and greater potency in animal model of inflammatory pain. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.04.105

文献信息

• Rapid, one-pot synthesis of α,α-disubstituted primary amines by the addition of Grignard reagents to nitriles under microwave heating conditions
  作者：Brian T. Gregg、Kathryn C. Golden、John F. Quinn、Hong-Jun Wang、Wei Zhang、Ruifang Wang、Francis Wekesa、Dmytro O. Tymoshenko

  DOI：10.1016/j.tetlet.2009.04.081

  日期：2009.7

  A series of α,α-disubstituted amines have been prepared in a simple and efficient one-pot procedure by the addition of Grignard reagents to a series of aliphatic, aromatic, and heteroaromatic nitriles. Key to this reported procedure is the unprecedented addition of the Grignard reagent to the nitrile under heating by microwave irradiation which both significantly improves reaction yields and reduces

  通过将格氏试剂添加到一系列脂族，芳族和杂芳族腈中，以简单有效的一锅法制备了一系列α，α-二取代胺。该报道方法的关键是在微波辐射加热下，将格氏试剂前所未有地添加到腈中，这既显着提高了反应产率，又缩短了反应时间。通常，格利雅（Grignard）加成反应在100°C下5-10分钟内完成，然后用硼氢化钠快速还原，得到目标胺。
• [EN] THERAPEUTIC METHODS<br/>[FR] MÉTHODES THÉRAPEUTIQUES
  申请人：GLAXO GROUP LTD

  公开号：WO2013085890A1

  公开（公告）日：2013-06-13

  The present invention relates to methods of treatment of diseases mediated by RORϒ.

  本发明涉及通过RORϒ介导的疾病治疗方法。
• SPIROPIPERIDINE GLYCINAMIDE DERIVATIVES
  申请人：Bissantz Caterina

  公开号：US20080171759A1

  公开（公告）日：2008-07-17

  In particular, the present invention is concerned with compounds of the general formula (I) wherein X, Y and R 1 to R 10 are as described herein. The compounds are V1a receptor antagonists. The invention also relates to the manufacture of compounds of formula I, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases.

  具体而言，本发明涉及一般式（I）中的化合物，其中X、Y和R1至R10如本文所述。这些化合物是V1a受体拮抗剂。该发明还涉及制备一般式I的化合物、含有它们的药物组合物以及它们用于治疗焦虑和抑郁症等疾病的用途。
• Di-aromatic substituted amides as inhibitors for GlyT-1
  申请人：Jolidon Synese

  公开号：US20080076806A1

  公开（公告）日：2008-03-27

  The present invention relates to compounds of formula I wherein R 1 , R 2 , R 3 , R 4 , R 5 , X, and n are as defined herein and the dotted line denotes an optional bond and pharmaceutically acceptable acid addition salts thereof. The compounds are useful in the treatment of neurological and neuropsychiatric disorders.

  本发明涉及式I的化合物，其中R1，R2，R3，R4，R5，X和n的定义如本文所述，点线表示可选键，以及其药学上可接受的酸盐。该化合物在神经系统和精神疾病的治疗中有用。
• DI-AROMATIC SUBSTITUTED AMIDES AS INHIBITORS FOR GLYT1
  申请人：F. Hoffmann-La Roche AG

  公开号：EP2066620A1

  公开（公告）日：2009-06-10