2-amino-4-(piperidin-1-yl)pyridine | 52311-35-0

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 2-amino-4-(piperidin-1-yl)pyridine
• 英文别名: 4-(piperidin-1-yl)-2-aminopyridine；2-amino-4-piperidinylpyridine；4-Piperidin-1-ylpyridin-2-amine
• CAS: 52311-35-0
• 化学式: C₁₀H₁₅N₃
• 分子量: 177.249
• InChiKey: IYUJNYOFNTWSFC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  13
• 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：
  42.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-amino-4-(piperidin-1-yl)pyridine 在 N,N'-二环己基碳二亚胺 、 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 4.0h， 生成 (S)-N-((S)-1-oxo-1-((4-(piperidin-1-yl)pyridin-2-yl)amino)-propan-2-yl)pyrrolidine-2-carboxamide
  参考文献：
  名称：

  Proline-based dipeptides as efficient organocatalysts for asymmetric aldol reactions in brine

  摘要：

  Simple N-proline-based dipeptides with two N-H groups in combination with 2,4-dinitrophenol (DNP) catalyze the direct asymmetric aldol reactions of aldehydes with a broad range of ketones to furnish the corresponding aldol products in high yields (up to 99%) and with high enantioselectivities (up to 97%) and diastereoselectivities (up to > 99:1, anti/syn) at room temperature and in brine. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetasy.2011.06.017
• 作为产物：
  描述：

  哌啶 、 2-氨基-4-氯吡啶 反应 48.0h， 以89%的产率得到2-amino-4-(piperidin-1-yl)pyridine
  参考文献：
  名称：

  手性 2-氨基-4-哌啶基吡啶衍生物的简单有效合成方法

  摘要：

  摘要 已开发出一种简便的方法来提供一系列新型手性 N-(4-(哌啶-1-基)吡啶-2-基)酰胺衍生物作为潜在的立体选择性催化剂。关键中间体2-氨基-4-哌啶基吡啶是通过2-氨基-4-氯吡啶与哌啶的亲核取代获得的，产率高达96%。L-脯氨酸和(R)-1,1'-双(2-萘酚)衍生物的合成获得了对映选择性的完全控制。图形概要

  DOI：

  10.1080/00397911.2011.565453

文献信息

• Heteroarylalkanoic acids as integrin receptor antagonists derivatives
  申请人：Boys L. Mark

  公开号：US20050043344A1

  公开（公告）日：2005-02-24

  The present invention relates to pharmaceutical compositions comprising compounds of the Formula I, or a pharmaceutically acceptable salt thereof, and methods of selectively inhibiting or antagonizing the α V β 3 and/or the α V β 5 integrin without significantly inhibiting the α V β 6 integrin.

  本发明涉及包含式I的化合物或其药学上可接受的盐的制药组合物，以及选择性地抑制或拮抗αVβ3和/或αVβ5整合素的方法，而不显著抑制αVβ6整合素。
• HETEROARYLALKANOIC ACIDS AS INTEGRIN RECEPTOR ANTAGONISTS
  申请人：Pharmacia Corporation

  公开号：EP1592421A1

  公开（公告）日：2005-11-09
• [EN] HETEROARYLALKANOIC ACIDS AS INTEGRIN RECEPTOR ANTAGONISTS<br/>[FR] ACIDES HETEROARYLALCANOIQUES EN TANT QU'ANTAGONISTES DU RECEPTEUR D'INTEGRINE
  申请人：PHARMACIA CORP

  公开号：WO2004058254A1

  公开（公告）日：2004-07-15

  The present invention relates to pharmaceutical compositions comprising compounds of the Formula I, or a pharmaceutically acceptable salt thereof, and methods of selectively inhibiting or antagonizing the ανβ3 and/or the ανβ5 integrin without significantly inhibiting the ανβ6 integrin.
• Proline-based dipeptides as efficient organocatalysts for asymmetric aldol reactions in brine
  作者：Hua Tian、Jun-long Gao、Hao Xu、Liang-Yu Zheng、Wen-Bo Huang、Qing-Wen Liu、Suo-Qin Zhang

  DOI：10.1016/j.tetasy.2011.06.017

  日期：2011.5

  Simple N-proline-based dipeptides with two N-H groups in combination with 2,4-dinitrophenol (DNP) catalyze the direct asymmetric aldol reactions of aldehydes with a broad range of ketones to furnish the corresponding aldol products in high yields (up to 99%) and with high enantioselectivities (up to 97%) and diastereoselectivities (up to > 99:1, anti/syn) at room temperature and in brine. (C) 2011 Elsevier Ltd. All rights reserved.
• Simple and Effective Synthetic Approach to Chiral 2-Amino-4-piperidinyl Pyridine Derivatives
  作者：Hua Tian、Qing-Wen Liu、Hao Xu、Wen-Bo Huang、Jian Lin、Suo-Qin Zhang

  DOI：10.1080/00397911.2011.565453

  日期：2012.9.15

  N-(4-(piperidin-1-yl)pyridin-2-yl)amide derivatives as potential stereoselective catalysts. The key intermediate, 2-amino-4-piperidinyl pyridine, was obtained by nucleophilic substitution of 2-amino-4-chloropyridine with piperidine in good yields (up to 96%). The total control of enantioselectivity was obtained for the synthesis of L-proline and (R)-1,1′-bi(2-naphthol) derivatives. GRAPHICAL ABSTRACT

  摘要 已开发出一种简便的方法来提供一系列新型手性 N-(4-(哌啶-1-基)吡啶-2-基)酰胺衍生物作为潜在的立体选择性催化剂。关键中间体2-氨基-4-哌啶基吡啶是通过2-氨基-4-氯吡啶与哌啶的亲核取代获得的，产率高达96%。L-脯氨酸和(R)-1,1'-双(2-萘酚)衍生物的合成获得了对映选择性的完全控制。图形概要