3-(哌啶-3-基)吡啶 | 31251-28-2

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 3-(哌啶-3-基)吡啶
• 英文名称: 3-(3-Pyridyl)piperidin
• 英文别名: 3-(Piperidin-3-yl)pyridine；3-piperidin-3-ylpyridine
• CAS: 31251-28-2
• 化学式: C₁₀H₁₄N₂
• 分子量: 162.235
• InChiKey: KLDGENGYOLDCCH-UHFFFAOYSA-N

物化性质

• 沸点：
  285.2±28.0 °C(Predicted)
• 密度：
  1.014±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  24.9
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 海关编码：
  2933990090
• 包装等级：
  III
• 危险类别：
  8
• 危险性防范说明：
  P261,P264,P270,P271,P280,P302+P352,P304+P340,P305+P351+P338,P310,P330,P332+P313,P362,P403+P233,P405,P501
• 危险品运输编号：
  1759
• 危险性描述：
  H302,H315,H318,H335

反应信息

• 作为反应物：
  描述：

  3-(哌啶-3-基)吡啶 、 3'-氯-4-氟苯丙酮 在 potassium carbonate 、 sodium iodide 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以5%的产率得到1-(4-fluorophenyl)-3-(3-pyridin-3-ylpiperidin-1-yl)propan-1-one
  参考文献：
  名称：

  Synthesis and evaluation of 3-aryl piperidine analogs as potent and efficacious dopamine D4 receptor agonists

  摘要：

  A series of 3-aryl piperidine analogs with 2-piperidinoalkylamino or 2-piperidinoalkyloxy fused bicyclic rings were prepared and found to be potent and efficacious human dopamine D-4 agonists. The synthesis and structure-activity relationship (SAR) studies that led to the identification of these compounds are discussed. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2005.04.060
• 作为产物：
  描述：

  N-叔丁氧羰基-3-哌啶酮 在 四(三苯基膦)钯 三氟乙酸 、 lithium diisopropyl amide 作用下， 以 四氢呋喃 、 正己烷 、 二氯甲烷 为溶剂， 反应 2.25h， 生成 3-(哌啶-3-基)吡啶
  参考文献：
  名称：

  Synthesis and evaluation of 3-aryl piperidine analogs as potent and efficacious dopamine D4 receptor agonists

  摘要：

  A series of 3-aryl piperidine analogs with 2-piperidinoalkylamino or 2-piperidinoalkyloxy fused bicyclic rings were prepared and found to be potent and efficacious human dopamine D-4 agonists. The synthesis and structure-activity relationship (SAR) studies that led to the identification of these compounds are discussed. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2005.04.060

文献信息

• PYRROLOTRIAZINE KINASE INHIBITORS
  申请人：Fink E. Brian

  公开号：US20080045496A1

  公开（公告）日：2008-02-21

  The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of such as TrkA, TrkB, TrkC, Jak2, Jak3 and CK2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.

  本发明提供了公式I的化合物以及药用可接受的盐类。公式I的化合物可以抑制诸如TrkA、TrkB、TrkC、Jak2、Jak3和CK2的酪氨酸激酶活性，从而使其作为抗增殖剂用于治疗癌症和其他疾病的有用性。
• [EN] OLIGONUCLEOTIDE COMPOSITIONS AND METHODS THEREOF<br/>[FR] COMPOSITIONS D'OLIGONUCLÉOTIDES ET PROCÉDÉS ASSOCIÉS
  申请人：WAVE LIFE SCIENCES LTD

  公开号：WO2021237223A1

  公开（公告）日：2021-11-25

  The present disclosure provides modified oligonucleotides and compositions and methods thereof. In some embodiments, provided technologies comprise modified sugars and/or modified internucleotidic linkages. In some embodiments, the present disclosure provides technologies for preparing modified oligonucleotides. In some embodiments, the present disclosure provides chirally controlled oligonucleotide compositions and methods for their preparation and uses.

  本公开提供了经修改的寡核苷酸及其组合物和方法。在某些实施方式中，提供的技术包括修改的糖或修改的核苷酸间连接。在某些实施方式中，本公开提供了用于制备修改的寡核苷酸的技术。在某些实施方式中，本公开提供了对手性控制的寡核苷酸组合物及其制备和用途的方法。
• A novel inhibitor of inducible NOS dimerization protects against cytokine-induced rat beta cell dysfunction
  作者：Linlin Zhong、Tuan Tran、Tyler D Baguley、Sang Jun Lee、Adam Henke、Andrew To、Sijia Li、Shan Yu、Fabio A Grieco、Jason Roland、Peter G Schultz、Decio L Eizirik、Nikki Rogers、Arnab K Chartterjee、Matthew S Tremblay、Weijun Shen

  DOI：10.1111/bph.14388

  日期：2018.9

  Background and PurposeBeta cell apoptosis is a major feature of type 1 diabetes, and pro‐inflammatory cytokines are key drivers of the deterioration of beta cell mass through induction of apoptosis. Mitochondrial stress plays a critical role in mediating apoptosis by releasing cytochrome C into the cytoplasm, directly activating caspase‐9 and its downstream signalling cascade. We aimed to identify new compounds that protect beta cells from cytokine‐induced activation of the intrinsic (mitochondrial) pathway of apoptosis.Experimental ApproachDiabetogenic media, composed of IL‐1β, IFN‐γ and high glucose, were used to induce mitochondrial stress in rat insulin‐producing INS1E cells, and a high‐content image‐based screen of small molecule modulators of Casp9 pathway was performed.Key ResultsA novel small molecule, ATV399, was identified from a high‐content image‐based screen for compounds that inhibit cleaved caspase‐9 activation and subsequent beta cell apoptosis induced by a combination of IL‐1β, IFN‐γ and high glucose, which together mimic the pathogenic diabetic milieu. Through medicinal chemistry optimization, potency was markedly improved (6–30 fold), with reduced inhibitory effects on CYP3A4. Improved analogues, such as CAT639, improved beta cell viability and insulin secretion in cytokine‐treated rat insulin‐producing INS1E cells and primary dispersed islet cells. Mechanistically, CAT639 reduced the production of NO by allosterically inhibiting dimerization of inducible NOS (iNOS) without affecting its mRNA levels.Conclusion and ImplicationsTaken together, these studies demonstrate a successful phenotypic screening campaign resulting in identification of an inhibitor of iNOS dimerization that protects beta cell viability and function through modulation of mitochondrial stress induced by cytokines.
• Plaquevent, Jean-Christophe; Chichaoui, Ilhame, Bulletin de la Societe Chimique de France, 1996, vol. 133, # 4, p. 369 - 379
  作者：Plaquevent, Jean-Christophe、Chichaoui, Ilhame

  DOI：——

  日期：——
• NEONICOTINE AND ISOMERIC PYRIDYLPIPERIDINES
  作者：C. R. Smith

  DOI：10.1021/ja01352a038

  日期：1931.1.1