芬哌丙烷 | 3540-95-2

• 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: 芬哌丙烷
• 中文别名: 二苯丙哌啶
• 英文名称: fenpiprane
• 英文别名: 1-(3,3-diphenylpropyl)piperidine；N-(3,3-diphenylpropyl)piperidine
• CAS: 3540-95-2
• 化学式: C₂₀H₂₅N
• 分子量: 279.425
• InChiKey: JXJPYHDHJZJWRI-UHFFFAOYSA-N

物化性质

• 熔点：
  41-42.5°
• 沸点：
  bp8 210-220°
• 密度：
  0.9328 (rough estimate)

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  21
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

安全信息

• 海关编码：
  2933399090
• 储存条件：
  2-8°C

反应信息

• 作为反应物：
  描述：

  芬哌丙烷 在 溶剂黄146 、 铂 作用下， 生成 1-(3-环己基-3-苯基丙基)哌啶
  参考文献：
  名称：

  Antispasmodics. N-(3-Phenylpropyl)-amines and 3-Amino-1-phenyl-1-propanols¹

  摘要：

  DOI：

  10.1021/ja01158a018
• 作为产物：
  描述：

  3,3-二苯基丙醇 在 氯化亚砜 、 苯 作用下， 生成 芬哌丙烷
  参考文献：
  名称：

  Diaryl nitrogenous heterocyclic alkylene compounds

  摘要：

  公开号：

  US02446522A1

文献信息

• Benzimidazolin-2-ylidene N-heterocyclic carbene complexes of ruthenium as a simple catalyst for the N-alkylation of amines using alcohols and diols
  作者：Siah Pei Shan、Xie Xiaoke、Boopathy Gnanaprakasam、Tuan Thanh Dang、Balamurugan Ramalingam、Han Vinh Huynh、Abdul Majeed Seayad

  DOI：10.1039/c4ra15398g

  日期：——

  for the alkylation of amines using alcohols as alkylating agents. Catalysts 1, 2 and 3a gave excellent yields of up to 99% for the alkylation of various amines using benzylic and aliphatic alcohols at 130 °C for 18 h under solventless conditions. Catalyst 3a bearing both phosphine and carbene ligands gave excellent yields of up to 98% for the synthesis of heterocyclic amines by double alkylation of primary

  简单的空气和湿气稳定的钌配合物1-3和3a是由易于获得的苯并环化的N-杂环卡宾配体（bimy =苯并咪唑啉-2-亚基）合成的。发现这些络合物是使用醇作为烷基化剂将胺烷基化的有效催化剂。催化剂1，2和3a中放弃的优异的产率至99％，使用苄和脂族醇各种胺的烷基化在130℃下为无溶剂的条件下18小时。催化剂3a含膦和卡宾配体的苯胺通过使用线性二醇对伯胺进行双烷基化合成杂环胺，可提供高达98％的优异收率。在无溶剂条件下，以更环保的方式证明了这些催化剂在药学上重要的胺的合成中的实用性。
• Hydroxylated nebivolol metabolites
  申请人：O'Donnell P. John

  公开号：US20070014733A1

  公开（公告）日：2007-01-18

  Hydroxylated nebivolol metabolites increase NO release from human endothelial cell preparations in a concentration dependent fashion following acute administration. In addition, hydroxylated nebivolol metabolites, including but not limited to 4-hydroxy-6,6′difluoro-, 4-hydroxy-5-phenol-6,6′difluoro-, and 4-hydroxy-8-pheno-6,6′difluoro-, have the ability to increase the capacity for NO release in human endothelial cells following chronic administration. This invention provides hydroxylated nebivolol metabolites and compositions comprising nebivolol and/or at least one hydroxylated metabolite of nebivolol and/or at least one additional compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof. In addition, this invention provides methods of treating and/or preventing vascular diseases by administering at least one hydroxylated metabolite of nebivolol that is capable of releasing a therapeutically effective amount of nitric oxide to a targeted site affected by the vascular disease. Also, this invention is directed to the treatment and/or prevention of migraine headaches administering at least one hydroxylated metabolite of nebivolol. This invention may also be used in conjunction with or as a single treatment of metabolic syndrome disorders.

  羟基化奈必洛尔代谢物在急性给药后以浓度依赖性方式增加人内皮细胞制剂的一氧化氮释放。此外，羟基化奈必洛尔代谢物，包括但不限于4-羟基-6,6'-二氟代-、4-羟基-5-苯酚-6,6'-二氟代-和4-羟基-8-苯并-6,6'-二氟代-，在慢性给药后能够增加人内皮细胞的一氧化氮释放能力。本发明提供了羟基化奈必洛尔代谢物和包含奈必洛尔和/或至少一种羟基化奈必洛尔代谢物和/或至少一种用于治疗心血管疾病的附加化合物的组合物，以及可药用的盐。此外，本发明还提供了通过给药至少一种能够释放治疗有效量的一氧化氮到受血管疾病影响的靶向部位的羟基化奈必洛尔代谢物来治疗和/或预防血管疾病的方法。本发明还涉及通过给药至少一种羟基化奈必洛尔代谢物来治疗和/或预防偏头痛。本发明还可以与治疗代谢综合征障碍的其他治疗联合使用，或作为单一治疗。
• [EN] TRIAZOLOBENZAZEPINES AS VASOPRESSIN V1A RECEPTOR ANTAGONISTS<br/>[FR] TRIAZOLOBENZAZÉPINES UTILISÉES EN TANT QU'ANTAGONISTES DU RÉCEPTEUR DE LA VASOPRESSINE V1A
  申请人：RICHTER GEDEON NYRT

  公开号：WO2019116324A1

  公开（公告）日：2019-06-20

  The present invention relates to 5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine derivatives of general formula (I) and/or salts thereof and/or geometric isomers thereof and/or stereoisomers thereof and/or enantiomers thereof and/or racemates thereof and/or diastereomers thereof and/or biologically active metabolites thereof and/or prodrugs thereof and/or solvates thereof and/or hydrates thereof and/or polymorphs thereof which are centrally and/or peripherally acting V1a receptor modulators, particularly V1a receptor antagonists. Additional subject of the present invention is the process for the preparation of the compounds and the intermediates of the preparation process as well. The invention also relates to the pharmaceutical compositions containing the compounds or together with one or more other active substances, as well as to the use in the treatment and/or prophylaxis of a disease or condition associated with V1a receptor function.

  本发明涉及一般式(I)的5,6-二氢-4H-[1,2,4]三唑并[4,3-a][1]苯并蒽啉衍生物和/或其盐和/或其几何异构体和/或其立体异构体和/或其对映异构体和/或其消旋体和/或其非对映异构体和/或其生物活性代谢物和/或其前药和/或其溶剂化合物和/或其水合物和/或其多晶形式，这些化合物是中枢和/或外周作用的V1a受体调节剂，特别是V1a受体拮抗剂。本发明的另一个主题是制备这些化合物的过程以及制备过程的中间体。该发明还涉及含有这些化合物或与一个或多个其他活性物质一起的药物组合物，以及在治疗和/或预防与V1a受体功能相关的疾病或症状中的用途。
• Hydroaminomethylation with Novel Rhodium–Carbene complexes: An Efficient Catalytic Approach to Pharmaceuticals
  作者：Moballigh Ahmed、Cathleen Buch、Lucie Routaboul、Ralf Jackstell、Holger Klein、Anke Spannenberg、Matthias Beller

  DOI：10.1002/chem.200601155

  日期：2007.2.2

  3-dimesitylimidazole-2-ylidenes the novel [RhCl(cod)(carbene)] complexes 1-5 have been synthesized, characterized, and tested in the hydroaminomethylation of aromatic olefins. The influence of different ligands and reaction parameters on the catalytic activity was investigated in detail applying 1,1-diphenylethylene and piperidine as a model system. The scope and limitations of the novel catalysts is shown in the

  从[Rh（cod）Cl}（2）]和1,3-二甲基咪唑-2-亚烷基开始，已经合成，表征和测试了新型[RhCl（cod）（carbene）]配合物1-5芳族烯烃。以1，1-二苯基乙烯和哌啶为模型体系，详细研究了不同配体和反应参数对催化活性的影响。在制备16种具有生物活性的1-氨基-3,3-二芳基丙烯中显示了新型催化剂的范围和局限性。通常，获得了高的化学和区域选择性以及所需产物的良好产率。
• [EN] HYDROXYINDALPINE DERIVATIVES AND THEIR MEDICAL USE<br/>[FR] DÉRIVÉS D'HYDROXYINDALPINE ET LEUR UTILISATION MÉDICALE
  申请人：TECH UNIVERSITÄT MÜNCHEN

  公开号：WO2014125084A1

  公开（公告）日：2014-08-21

  The present invention relates to hydroxyindalpine derivatives of formula (I) as defined herein and pharmaceutical compositions comprising these compounds, as well as their medical use, particularly in the treatment or prevention of gastrointestinal diseases/disorders, such as constipation and functional dyspepsia.

  本发明涉及公式（I）中定义的羟基因达尔平衍生物，以及包含这些化合物的药物组合物，以及它们在医学上的用途，特别是在治疗或预防胃肠道疾病/紊乱方面，如便秘和功能性消化不良。