1-[双-(4-氟苯基)-甲基]-哌啶 | 252644-60-3

• 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: 1-[双-(4-氟苯基)-甲基]-哌啶
• 英文名称: 1-(bis(4-fluorophenyl)methyl)piperidine
• 英文别名: N-(4,4'-difluorobenzhydryl)piperidine；1-[Bis(4-fluorophenyl)methyl]piperidine
• CAS: 252644-60-3
• 化学式: C₁₈H₁₉F₂N
• 分子量: 287.352
• InChiKey: WTOSWPBNFCJVHA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-羟基-1.3-二苯基-2-(4-甲氧基-苯基)-丙烷 、 1-[双-(4-氟苯基)-甲基]-哌啶 、 草酸 、 甲醇 以 乙酸乙酯 为溶剂， 生成 (2S)-(-)-1-(4-indolyloxy)-3-(4-bis(4-fluorophenyl)methylpiperidin-1-yl)-2-propanol ethanedioate
  参考文献：
  名称：

  Compounds having effects on serotonin-related systems

  摘要：

  一系列杂氧基烷胺化合物是治疗与血清素再摄取和血清素1.sub.A受体相关或受其影响的疾病的有效药物。这些化合物特别适用于缓解尼古丁和烟草戒断症状，并用于治疗抑郁症和其他需要使用血清素再摄取抑制剂的疾病。

  公开号：

  US05741789A1
• 作为产物：
  描述：

  哌啶 在 2,2'-联吡啶 、 copper(I) bromide 作用下， 以 1,2-二氯乙烷 、 苯 为溶剂， 反应 18.0h， 生成 1-[双-(4-氟苯基)-甲基]-哌啶
  参考文献：
  名称：

  Copper(I)-catalyzed coupling reaction of aryl boronic acids with N,O-acetals and N,N-aminals under atmosphere leading to α-aryl glycine derivatives and diarylmethylamine derivatives

  摘要：

  We demonstrated a copper(I)-catalyzed coupling reaction of aryl boronic acids with N,O-acetals and N,N-aminals leading to the synthesis of alpha-aryl glycines and diarylmethylamines. Under an ambient atmosphere, this catalytic system could be applied to the activation of a C(sp(3))-O bond of N,O-acetals with an ester and an aryl group, or without a coordinating substituent, as well as to a C(sp(3))-N bond of N,N-aminals. (C) 2015 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2015.05.068

文献信息

• Synthesis of Tertiary<i>sec</i>-Alkylamines by the Addition of Grignard Reagents to<i>N</i>,<i>N</i>-Dialkylformamides Mediated by Ti(O<i>i</i>Pr)₄and Me₃SiCl
  作者：Olesya Tomashenko、Viktor Sokolov、Alexander Tomashevskiy、Herwig A. Buchholz、Urs Welz-Biermann、Vladimir Chaplinski、Armin de Meijere

  DOI：10.1002/ejoc.200800629

  日期：2008.10

  A number of tertiary sec-alkylamines (22 examples, 29–80 % yield) have been prepared according to a simple one-pot procedure by the addition of Grignard reagents to N,N-dialkylformamides in the presence of Ti(OiPr)4 and Me3SiCl. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2008)

  在 Ti(OiPr)4 存在下，通过将格氏试剂加入 N,N-二烷基甲酰胺中，通过简单的一锅法制备了许多叔仲烷基胺（22 个实例，29-80% 产率）和Me3SiCl。(© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2008)
• Compounds having effects on serotonin-related systems
  申请人：Eli Lilly and Company

  公开号：US05614523A1

  公开（公告）日：1997-03-25

  A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.

  一系列的杂氧基烷胺是有效的药物，用于治疗与血清素再摄取和血清素1.sub.A受体有关或受其影响的病症。这些化合物特别适用于缓解尼古丁和烟草戒断症状，并用于治疗抑郁症和其他需要使用血清素再摄取抑制剂的病症。
• Indolyl-3-glyoxylic acid derivatives having antitumor action
  申请人：Nickel Bernd

  公开号：US20080027110A1

  公开（公告）日：2008-01-31

  The invention relates to the use of N-substituted indole-3-glyoxylamides of the general formula I as antitumor agents and to a pharmaceutical composition having antitumor action, characterized in that it contains at least one of the compounds of the general formula 1, if appropriate also in the form of the physiologically tolerable acid addition salts or N-oxides. Furthermore, the invention also includes antitumor agents comprising as active compound one or more N-substituted indole-3-glyoxylamides according to the general formula 1 and, if appropriate, their physiologically tolerable acid addition salts and, if possible, N-oxides and a pharmaceutically utilizable carrier and/or diluent or auxiliary substance in the form of tablets, coated tablets, capsules, solutions for infusion or ampoules, suppositories, patches, powder preparations which can be employed by inhalation, suspensions, creams and ointments.

  本发明涉及使用一般式I的N-取代吲哚-3-甘氧酰胺作为抗肿瘤剂，以及具有抗肿瘤作用的药物组合物，其特征在于至少含有一种一般式1的化合物，如适当，还可以是生理耐受的酸加成盐或N-氧化物的形式。此外，本发明还包括作为活性化合物的一种或多种N-取代吲哚-3-甘氧酰胺的抗肿瘤剂，以及它们的生理耐受的酸加成盐和可能的N-氧化物，以及在片剂、包衣片剂、胶囊、输注溶液或安瓿、栓剂、贴片、可通过吸入使用的粉剂制剂、悬浮液、乳霜和软膏等药物可利用载体和/或稀释剂或辅助物质的形式。
• 6,6-Bicyclic Ring Substituted Heterobicyclic Protein Kinase Inhibitors
  申请人：Arnold Lee D.

  公开号：US20120077979A1

  公开（公告）日：2012-03-29

  Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , R 1 , and Q 1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.

  该式化合物及其药学上可接受的盐，其中X1、X2、X3、X4、X5、X6、X7、R1和Q1的定义详见本文，可以抑制IGF-1R酶，用于治疗和/或预防增生性疾病，如癌症、炎症、银屑病、过敏/哮喘、免疫系统疾病和病症、中枢神经系统疾病和病症。
• METHODS, COMPOSITIONS, AND KITS FOR THE TREATMENT OF CANCER
  申请人：Haggerty Timothy J.

  公开号：US20140335050A1

  公开（公告）日：2014-11-13

  The invention features methods, compositions, and kits for the administration of an HSP90 inhibitor, OBAA, flunarizine, aphidicolin, damnacanthal, dantrolene, or an analog thereof, alone, or in combination with, e.g., a TAA, an antigen-binding scaffold (e.g., an antibody, a soluble T cell receptor, or a chimeric receptor) specific for a TAA, a cell (e.g., a white blood cell that targets a cancer cell), and/or an IFN-β receptor agonist or an IFN-γ receptor agonist, for the treatment of cancer.