4-(4-methoxyphenyl)-1-methylpiperidine | 740789-86-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 4-(4-methoxyphenyl)-1-methylpiperidine
• CAS: 740789-86-0
• 化学式: C₁₃H₁₉NO
• 分子量: 205.3
• InChiKey: YJJIYWITNWIECO-UHFFFAOYSA-N

物化性质

• 沸点：
  296.9±40.0 °C(Predicted)
• 密度：
  0.998±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  12.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-(4-methoxyphenyl)-1-methylpiperidine 在 sodium hydroxide 、 三氟化硼-二甲醚络合物 作用下， 以 甲醇 、 二氯甲烷 为溶剂， 反应 12.0h， 生成 (E)-3-(2-chlorophenyl)-1-[2-methoxy-5-(1-methylpiperidin-4-yl)phenyl]prop-2-en-1-one
  参考文献：
  名称：

  Antiproliferative properties of piperidinylchalcones

  摘要：

  Methoxylated chalcones bearing N-methylpiperidinyl substituents oil ring A inhibited the growth of human tumour cell lines (MCF, HCT 116, and Jurkat) at IC50 values or < 5 mu M. Investigations oil a representative member (12) showed that antiproliferative activity was linked to the disruption of the cell cycle at G1 and G2/M phases. The effect was concentration dependent and was evident at the approximate IC50 of 12. Down regulation of cell cycle regulatory components (CDK4, cyclin B, E2F, and phosphorylated Rb) were observed under similar conditions. Methoxylated chalconcs without the piperidinyl substituent were found to exert equally potent and selective antiproliferative activity against HCT 116 tumour cells but did not interfere with cell cycle progression at their IC50 concentrations. The presence of the piperidinyl substituent in the chalcone template is proposed to lend specificity to the mechanism of antiproliferative activity, in addition to promoting a more desirable physicochemical profile. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2005.08.006
• 作为产物：
  描述：

  N-甲基-4-哌啶酮 在 palladium on activated charcoal 盐酸 、 氢气 、 溶剂黄146 作用下， 以 水 为溶剂， 20.0~100.0 ℃ 、275.79 kPa 条件下， 反应 3.0h， 生成 4-(4-methoxyphenyl)-1-methylpiperidine
  参考文献：
  名称：

  Antiproliferative properties of piperidinylchalcones

  摘要：

  Methoxylated chalcones bearing N-methylpiperidinyl substituents oil ring A inhibited the growth of human tumour cell lines (MCF, HCT 116, and Jurkat) at IC50 values or < 5 mu M. Investigations oil a representative member (12) showed that antiproliferative activity was linked to the disruption of the cell cycle at G1 and G2/M phases. The effect was concentration dependent and was evident at the approximate IC50 of 12. Down regulation of cell cycle regulatory components (CDK4, cyclin B, E2F, and phosphorylated Rb) were observed under similar conditions. Methoxylated chalconcs without the piperidinyl substituent were found to exert equally potent and selective antiproliferative activity against HCT 116 tumour cells but did not interfere with cell cycle progression at their IC50 concentrations. The presence of the piperidinyl substituent in the chalcone template is proposed to lend specificity to the mechanism of antiproliferative activity, in addition to promoting a more desirable physicochemical profile. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2005.08.006

文献信息

• [EN] 3-PHENYLSULPHONYL-QUINOLINE DERIVATIVES AS AGENTS FOR TREATING PATHOGENIC BLOOD VESSELS DISORDERS<br/>[FR] DÉRIVÉS DE 3-PHÉNYLSULFONYL-QUINOLÉINE EN TANT QU'AGENTS POUR LE TRAITEMENT DE TROUBLES DES VAISSEAUX SANGUINS PATHOGÈNES
  申请人：UNIV CALIFORNIA

  公开号：WO2021076886A1

  公开（公告）日：2021-04-22

  The disclosure provides compounds, and compositions, including pharmaceutical compositions, kits that include the compounds, and methods of using (or administering) and making the compounds. The disclosure further provides compounds or compositions thereof for use in a method of modulating PLXDC1 (TEM7) and/or PLXDC2 or killing pathogenic blood vessles. The disclosure further provides compounds or compositions thereof for use in a method of treating a disease, disorder, or condition that is mediated, at least in part, by PEDF receptors or by angiogenesis.

  该披露提供了化合物和组合物，包括药物组合物、包含这些化合物的试剂盒，以及使用（或给药）和制备这些化合物的方法。该披露进一步提供了用于调节PLXDC1（TEM7）和/或PLXDC2或杀灭病原性血管的方法中的化合物或其组合物。该披露还提供了用于治疗由PEDF受体或血管生成至少部分介导的疾病、紊乱或状况的方法中的化合物或其组合物。
• [EN] NOVEL COMPOUNDS SUITABLE FOR THE TREATMENT OF DYSLIPIDEMIA<br/>[FR] NOUVEAUX COMPOSÉS APPROPRIÉS POUR LE TRAITEMENT DE LA DYSLIPIDÉMIE
  申请人：CADILA HEALTHCARE LTD

  公开号：WO2021130723A1

  公开（公告）日：2021-07-01

  The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation The present invention is directed towards compounds which can be useful in treating diseases such as Hyperlipidemia and also have a beneficial effect on lowering cholesterol.

  本发明涉及一般式（I）的化合物，它们的互变异构体，立体异构体，药学上可接受的盐，含有它们的药物组合物，它们的制备方法，这些化合物在医学上的应用以及其制备中涉及的中间体。本发明针对的是可以用于治疗高脂血症等疾病并且对降低胆固醇有益的化合物。
• ALPHA-SYNUCLEIN LIGANDS
  申请人：Washington University

  公开号：US20170189566A1

  公开（公告）日：2017-07-06

  The present invention generally relates to various compounds that are useful as α-synuclein ligands. The invention further relates to methods of using these compounds and their radiolabeled analogs for the detection of synucleinopathies, including Parkinson's disease (PD).

  本发明通常涉及作为α-突触核蛋白配体有用的各种化合物。该发明进一步涉及使用这些化合物及其放射标记类似物用于检测突触核蛋白病，包括帕金森病（PD）的方法。
• Visible‐Light‐Promoted Iron‐Catalyzed C(sp ² )–C(sp ³ ) Kumada Cross‐Coupling in Flow
  作者：Xiao‐Jing Wei、Irini Abdiaj、Carlo Sambiagio、Chenfei Li、Eli Zysman‐Colman、Jesús Alcázar、Timothy Noël

  DOI：10.1002/anie.201906462

  日期：2019.9.9

  A continuous‐flow, visible‐light‐promoted method has been developed to overcome the limitations of iron‐catalyzed Kumada–Corriu cross‐coupling reactions. A variety of strongly electron rich aryl chlorides, previously hardly reactive, could be efficiently coupled with aliphatic Grignard reagents at room temperature in high yields and within a few minutes’ residence time, considerably enhancing the applicability

  为了克服铁催化的Kumada-Corriu交叉偶联反应的局限性，开发了一种连续流，可见光促进的方法。可以在室温下以高收率和数分钟的停留时间，在室温下与脂肪族格氏试剂有效地偶联各种以前几乎没有反应性的强电子富集的芳基氯化物，从而大大提高了这种铁催化反应的适用性。该协议的鲁棒性已在数克规模上得到了证明，从而为将来的药物应用提供了潜力。
• Pyrrolo Pyrimidines as Agents for the Inhibition of Cystein Proteases
  申请人：Betschart Claudia

  公开号：US20090054467A1

  公开（公告）日：2009-02-26

  The invention provides compounds of Formula I or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors.

  本发明提供了公式I的化合物，或其药理学上可接受的盐或酯，其中符号具有定义的含义，这些化合物是卡特普西林K的抑制剂，并在药学上用于治疗与卡特普西林K有关的疾病和医疗条件，例如各种疾病，包括炎症，类风湿性关节炎，骨关节炎，骨质疏松和肿瘤。