1-(3-甲基吡啶-2-基)哌啶-4-酮 | 1057263-76-9

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 1-(3-甲基吡啶-2-基)哌啶-4-酮
• 英文名称: 1-(3-methylpyridin-2-yl)piperidin-4-one
• CAS: 1057263-76-9
• 化学式: C₁₁H₁₄N₂O
• 分子量: 190.245
• InChiKey: SXDCLJYHEZVTPI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  33.2
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-苯基双(三氟甲烷磺酰)亚胺 、 1-(3-甲基吡啶-2-基)哌啶-4-酮 在 lithium hexamethyldisilazane 作用下， 以 四氢呋喃 为溶剂， 反应 2.08h， 生成 [1-(3-methylpyridin-2-yl)-3,6-dihydro-2H-pyridin-4-yl] trifluoromethanesulfonate
  参考文献：
  名称：

  Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists

  摘要：

  A series of 1,2,3,6-tetrahydropyridyl-4-carboxamides, exemplified by 6, have been synthesized and evaluated for in vitro TRPV1 antagonist activity, and in vivo analgesic activity in animal pain models. The tetrahydropyridine 6 is a novel TRPV1 receptor antagonist that potently inhibits receptor-mediated Ca2+ influx in vitro induced by several agonists, including capsaicin, N-arachidonoyldopamine (NADA), and low pH. This compound penetrates the CNS and shows potent anti-nociceptive effects in a broad range of animal pain models upon oral dosing due in part to its ability to antagonize both central and peripheral TRPV1 receptors. The SAR leading to the discovery of 6 is presented in this report. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2008.08.005
• 作为产物：
  描述：

  8-(3-Methylpyridin-2-yl)-1,4-dioxa-8-azaspiro[4.5]decane 在 盐酸 作用下， 以 水 为溶剂， 反应 6.0h， 生成 1-(3-甲基吡啶-2-基)哌啶-4-酮
  参考文献：
  名称：

  [EN] TETRAHYDROPYRIDINE CARBOXAMIDE DERIVATIVES AS TRPVL ANTAGONISTS
  [FR] DÉRIVÉS AMIDES UTILISÉS COMME ANTAGONISTES DES TRPV1

  摘要：

  公开号：

  WO2009023539A3

文献信息

• AMIDE DERIVATIVES AS TRPV1 ANTAGONISTS
  申请人：Vasudevan Anil

  公开号：US20090062345A1

  公开（公告）日：2009-03-05

  The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R 1 , R 2 , and R 3 , are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.

  本发明涉及式(I)化合物，或其药学上可接受的盐、前药、前药盐或其组合物，其中R1、R2和R3在说明书中有定义。还公开了包含这些化合物的组合物以及使用这些化合物和组合物治疗疾病和疾患的方法。
• Biaryl Compounds Useful as Agonists of the Gpr38 Receptor
  申请人：MacDonald Gregor James

  公开号：US20080306083A1

  公开（公告）日：2008-12-11

  The present invention relates to novel biaryl derivatives such as compounds of formula (I), which have activity as agonists of the GPR38 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of gastrointestinal disorders.

  本发明涉及新型联苯衍生物，例如式（I）化合物，其具有作为GPR38受体激动剂的活性，以及在治疗胃肠道疾病中使用这种化合物或其制剂的药物组合物。
• TETRAHYDROPYRIDINE CARBOXAMIDE DERIVATIVES AS TRPVL ANTAGONISTS
  申请人：Abbott Laboratories

  公开号：EP2185538A2

  公开（公告）日：2010-05-19
• US7998982B2
  申请人：——

  公开号：US7998982B2

  公开（公告）日：2011-08-16
• US7964602B2
  申请人：——

  公开号：US7964602B2

  公开（公告）日：2011-06-21