2,6-dimethyl-N-formylpiperidine | 20722-50-3

• 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: 2,6-dimethyl-N-formylpiperidine
• 英文别名: 2,6-Dimethylpiperidine-1-carbaldehyde
• CAS: 20722-50-3
• 化学式: C₈H₁₅NO
• 分子量: 141.213
• InChiKey: ZZSRDYOYTXLWMU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.88
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  二氧化碳 、 2,6-二甲基哌啶 在 1,2-bis(diisopropylphosphino)benzene 、 copper(II) acetate monohydrate 作用下， 以 1,4-二氧六环 为溶剂， 80.0 ℃ 、101.33 kPa 条件下， 反应 30.0h， 以47%的产率得到2,6-dimethyl-N-formylpiperidine
  参考文献：
  名称：

  铜-二膦配合物催化剂，用于在1个大气压的二氧化碳下用聚甲基氢硅氧烷对胺进行N-甲酰化反应†

  摘要：

  在1个大气压的CO 2下，使用铜-二膦配合物作为均相催化剂与聚甲基氢硅氧烷（PMHS）进行多种胺的N-甲酰化反应。在反应中哌啶，例如，营业额（TON）在23小时内达到11700，甲酰化产物的收率为90％。该TON值远远高于已报道的催化剂，该催化剂用于在1个大气压的CO 2下用氢硅烷对胺进行甲酰化。与与丙基链连接的二齿配体和单齿配体相比，具有邻亚苯基结构的膦的Cu配合物充当了甲酰化的良好配体。在这些二膦中，具有烷基官能团的配体，例如异丙基和环己基，比苯基产生更好的结果。发现不仅环状仲胺，而且线性仲胺以及芳族和脂族伯胺也是反应性底物。如果是2,2,6,6-四甲基哌啶-4-胺，甲酰化区域选择性地进行。使用[Me 2 NCO 2 ] [Me 2 NH 2 ]从另一个实验中提出了催化反应途径。

  DOI：

  10.1039/c3cy00375b

文献信息

• Amine formylation via carbon dioxide recycling catalyzed by a simple and efficient heterogeneous palladium catalyst
  作者：Xinjiang Cui、Yan Zhang、Youquan Deng、Feng Shi

  DOI：10.1039/c3cc46427j

  日期：——

  Al2O3-NR support through a two-step process that involves hydrothermal synthesis of Al2O3-NRs followed by reductive-deposition of palladium. This catalyst showed high activity in the catalytic formylation of amines by CO2-H2 under mild conditions with up to 96% yield.

  一种简单有效的Pd / Al2O3-NR-RD催化剂，是通过两步过程将钯沉积在形状可控的Al2O3-NR载体上而制备的，该过程涉及水热合成Al2O3-NRs，然后进行钯的还原沉积。该催化剂在温和条件下通过CO2-H2催化胺的甲酰化反应具有很高的活性，收率高达96％。
• [EN] 4-SUBSTITUTED PIPERIDINE DERIVATIVES<br/>[FR] DERIVES DE PIPERIDINE SUBSTITUES EN POSITION 4
  申请人：BIOAXONE THERAPEUTIQUE INC

  公开号：WO2005080394A1

  公开（公告）日：2005-09-01

  Substituted piperidine compounds represented by the structure I are provided, wherein each of Rla, R1b, R1c, R1d, Rle, R1f, R1g, R1h, R2, R2A, R3, R4, A, X, a, x, and n is as defined in the specification. Substituted piperidine compounds of structure I may permeate or penetrate across a nerve cell membrane into the interior of a nerve cell, may inhibit intracellular Rho kinase enzyme found in nerve cells in mammals, and may find utility in repair of damaged nerves in the central and peripheral nervous system of such mammals. These compounds may induce the regeneration or growth of neurites in mammalian nerve cells and may thereby induce regeneration of damaged or diseased nerve tissue. These compounds also find additional utility as antagonists of the enzyme Rho kinase in treatment of disease states in which Rho kinase is implicated. Pharmaceutical compositions containing these substituted piperidine compounds may be useful to promote neurite growth and in the treatment of diseases in which Rho kinase inhibition is indicated.

  提供了由结构I表示的取代哌啶化合物，其中Rla、R1b、R1c、R1d、Rle、R1f、R1g、R1h、R2、R2A、R3、R4、A、X、a、x和n中的每一个如规范中定义。结构I的取代哌啶化合物可能渗透或穿过神经细胞膜进入神经细胞内部，可能抑制哺乳动物神经细胞中的细胞内Rho激酶酶，并可能在这些哺乳动物的中枢和外周神经系统中修复受损神经时发挥作用。这些化合物可能诱导哺乳动物神经细胞中神经突起的再生或生长，从而诱导受损或患病神经组织的再生。这些化合物还可作为Rho激酶酶拮抗剂在治疗涉及Rho激酶的疾病状态中发挥额外作用。含有这些取代哌啶化合物的药物组合物可能有助于促进神经突起的生长，并在需要Rho激酶抑制的疾病治疗中发挥作用。
• Fused-ring compounds and use thereof as drugs
  申请人：Japan Tobacco Inc.

  公开号：US20030050320A1

  公开（公告）日：2003-03-13

  The present invention provides a fused ring compound of the following formula [I] 1 wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and a therapeutic agent for hepatitis C, which contains this compound. The compound of the present invention shows an anti-hapatitis C virus (HCV) action based on the HCV polymerase inhibitory activity, and is useful as a therapeutic agent or prophylactic agent for hepatitis C.

  本发明提供了以下式子的融合环化合物I1，其中每个符号如规范所定义，其药用盐，以及包含该化合物的治疗丙型肝炎的治疗剂。本发明的化合物显示出基于HCV聚合酶抑制活性的抗丙型肝炎病毒（HCV）作用，并且可用作治疗或预防丙型肝炎的药物。
• 6- (Heterocyclyl-substituted Benzyl) -4-Oxoquinoline Compound and Use Thereof as HIV Integrase Inhibitor
  申请人：SATOH Motohide

  公开号：US20080207618A1

  公开（公告）日：2008-08-28

  The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical composition, an anti-HIV agent and an HIV integrase inhibitor containing such compound. The compound of the present invention has an HIV integrase inhibitory activity, and is useful as an anti-HIV agent, or as an agent for the prophylaxis or treatment of AIDS. In addition, by the combined use with other anti-HIV agents such as a protease inhibitor, a reverse transcriptase inhibitor and the like, it can be a more effective anti-HIV agent. Because it shows integrase-specific high inhibitory activity, the compound can be a pharmaceutical agent safe on human body, which causes only a fewer side effects.

  本发明涉及以下式[I]所表示的化合物，其中每个符号如规范中所定义，或其药学上可接受的盐，或其溶剂合物，以及含有此类化合物的药物组合物，抗HIV药物和HIV整合酶抑制剂。本发明的化合物具有HIV整合酶抑制活性，并可用作抗HIV药物，或用作艾滋病的预防或治疗药物。此外，通过与其他抗HIV药物（如蛋白酶抑制剂、逆转录酶抑制剂等）的联合使用，可以使其成为更有效的抗HIV药物。由于它显示出整合酶特异性的高抑制活性，该化合物可以成为对人体安全的药物，仅引起较少的副作用。
• 4-Substituted piperidine derivatives
  申请人：McKerracher Lisa

  公开号：US20050272751A1

  公开（公告）日：2005-12-08

  Substituted piperidine compounds represented by the structure I are provided, wherein each of R 1a , R 1b , R 1c , R 1d , R 1e , R 1f , R 1g , R 1h , R 2 , R 2A , R 3 , R 4 , A, X, a, x and n is as defined in the specification. Substituted piperidine compounds of structure I may permeate or penetrate across a nerve cell membrane into the interior of a nerve cell, may inhibit intracellular Rho kinase enzyme found in nerve cells in mammals, and may find utility in repair of damaged nerves in the central and peripheral nervous system of such mammals. These compounds may induce the regeneration or growth of neurites in mammalian nerve cells and may thereby induce regeneration of damaged or diseased nerve tissue. These compounds also find additional utility as antagonists of the enzyme Rho kinase in treatment of disease states in which Rho kinase is implicated. Pharmaceutical compositions containing these substituted piperidine compounds may be useful to promote neurite growth and in the treatment of diseases in which Rho kinase inhibition is indicated.

  提供了由结构式I表示的取代哌啶化合物，其中R1a、R1b、R1c、R1d、R1e、R1f、R1g、R1h、R2、R2A、R3、R4、A、X、a、x和n的定义如规范中所述。结构式I的取代哌啶化合物可以渗透或穿过神经细胞膜进入神经细胞内部，可以抑制哺乳动物神经细胞中发现的细胞内Rho激酶酶，并可用于修复哺乳动物中心和周围神经系统中的受损神经。这些化合物可以诱导哺乳动物神经细胞的轴突再生或生长，从而诱导受损或患病的神经组织再生。这些化合物还可作为Rho激酶酶拮抗剂，在治疗涉及Rho激酶酶的疾病状态中发现其他用途。含有这些取代哌啶化合物的制药组合物可用于促进神经轴突生长，并用于治疗需要Rho激酶抑制的疾病。