1-(2-Oxo-propyl)-piperidin-2-one | 138196-47-1

• 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: 1-(2-Oxo-propyl)-piperidin-2-one
• 英文别名: 1-(2-Oxopropyl)piperidin-2-one
• CAS: 138196-47-1
• 化学式: C₈H₁₃NO₂
• 分子量: 155.197
• InChiKey: XEISXIKNIZWXQN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  37.4
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-(2-Oxo-propyl)-piperidin-2-one 在 4-二甲氨基吡啶 、 甲基磺酰氯 、 三乙胺 、 lithium diisopropyl amide 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 0.5h， 生成 1-{(E)-5-[4-(2-Isopropoxy-phenyl)-piperazin-1-yl]-2-oxo-pent-3-enyl}-piperidin-2-one
  参考文献：
  名称：

  Novel arylpiperazines as selective α 1 -adrenergic receptor antagonists

  摘要：

  A novel series of arylpiperazines has been synthesized and identified as antagonists of alpha(1a) adrenergic receptor (alpha(1a)-AR) implicated in benign prostatic hyperplasia. These compounds selectively bind to membrane bound alpha(1a)-AR with K(i)s as low as 0.66 nM. As such, these potentially represent a viable treatment for BPH without the side effects associated with known alpha(1)-adrenergic antagonists. (C) 2000 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(00)00169-4
• 作为产物：
  描述：

  1-(2-methylallyl)piperidin-2-one 在 sodium periodate 、 四氧化锇 作用下， 以 1,4-二氧六环 为溶剂， 生成 1-(2-Oxo-propyl)-piperidin-2-one
  参考文献：
  名称：

  Novel arylpiperazines as selective α 1 -adrenergic receptor antagonists

  摘要：

  A novel series of arylpiperazines has been synthesized and identified as antagonists of alpha(1a) adrenergic receptor (alpha(1a)-AR) implicated in benign prostatic hyperplasia. These compounds selectively bind to membrane bound alpha(1a)-AR with K(i)s as low as 0.66 nM. As such, these potentially represent a viable treatment for BPH without the side effects associated with known alpha(1)-adrenergic antagonists. (C) 2000 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(00)00169-4

文献信息

• HYDROXYMETHYL PYRROLIDINES AS BETA 3 ADRENERGIC RECEPTOR AGONISTS
  申请人：Berger Richard

  公开号：US20090253705A1

  公开（公告）日：2009-10-08

  The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.

  本发明提供了式(I)的化合物，其药物组成物以及使用该化合物在治疗或预防由β3-肾上腺素受体激活介导的疾病的方法。
• Palladium(<scp>II</scp>)-catalysed oxidation of carbon–carbon double bonds of allylic compounds with molecular oxygen; regioselective formation of aldehydes
  作者：Takahiro Hosokawa、Shunji Aoki、Minoru Takano、Takatoshi Nakahira、Yoshinori Yoshida、Shun-Ichi Murahashi

  DOI：10.1039/c39910001559

  日期：——

  Treatment of N-allylamides 1a–c and lactams 1d–f with molecular oxygen in the presence of [PdCl2(MeCN)2]–CuCl catalyst in anhydrous 1,2-dichloroethane containing hexamethylphosphoric triamide gives the corresponding aldehydes 2 regioselectively, while methyl ketones 3 become the major products in the presence of water.

  N-烯丙基酰胺1a–c和内酰胺1d–f在[PdCl2(MeCN)2]–CuCl催化剂存在下，于无水1,2-二氯乙烷含六甲基磷酰胺中与分子氧反应，可以区域选择性地得到相应的醛2，而在水的存在下，主要的产物是甲基酮3。
• PROTEOSTASIS REGULATORS
  申请人：Foley Megan

  公开号：US20120316193A1

  公开（公告）日：2012-12-13

  The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.

  本发明涉及具有化学式(Ia-Ie)、(II)、(IIIa-IIId)、(IVa-IVc)、(Va-Vb)、(VIa-VIe)、(VII)、(VIIIa-VIIIc)和(IX)的化合物，以及这些化合物的药用可接受盐、前药和溶剂合物，以及这些化合物的任何组合物，并且用于治疗与蛋白质稳态功能紊乱相关的疾病的方法，包括有效量的这些化合物。
• [EN] HYDROXYMETHYL PYRROLIDINES AS BETA 3 ADRENERGIC RECEPTOR AGONISTS<br/>[FR] HYDROXYMÉTHYL PYRROLIDINES EN TANT QU'AGONISTES DE RÉCEPTEUR BÊTA 3 ADRÉNERGIQUE
  申请人：MERCK & CO INC

  公开号：WO2009124167A1

  公开（公告）日：2009-10-08

  The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.

  本发明提供了化合物(I)、其制药组合物以及使用它们治疗或预防由β3肾上腺素能受体激活介导的疾病的方法。
• Thiophene substituted piperazines useful in the treatment of benign prostatic hyperplasia
  申请人：Ortho-McNeil Pharmaceutical, Inc.

  公开号：EP1273572A1

  公开（公告）日：2003-01-08

  This invention relates to a series of heterocyclic substituted piperazines of Formula (I), pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the α-la adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this disease.

  本发明涉及一系列式（I）的杂环取代哌嗪类化合物、含有这些化合物的药物组合物以及用于制造这些化合物的中间体。本发明的化合物可选择性地抑制与 α-la 肾上腺素能受体的结合，该受体与良性前列腺增生症有关。因此，本发明化合物可用于治疗这种疾病。