2-甲氧基-5-(吡啶-4-基)吡啶-3-胺 | 91041-36-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: 2-甲氧基-5-(吡啶-4-基)吡啶-3-胺
• 英文名称: 6-methoxy-[3,4'-bipyridin]-5-amine
• 英文别名: [3,4'-Bipyridin]-5-amine, 6-methoxy-；2-methoxy-5-pyridin-4-ylpyridin-3-amine
• CAS: 91041-36-0
• 化学式: C₁₁H₁₁N₃O
• 分子量: 201.228
• InChiKey: SEBMZUMTPNGZEV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  61
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-甲氧基-5-(吡啶-4-基)吡啶-3-胺 在 potassium carbonate 、 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 为溶剂， 生成 (R)-2-hydroxy-N-(6-methoxy-[3,4′-bipyridin]-5-yl)-3-phenylpropanamide
  参考文献：
  名称：

  Phenylalanine derivatives as GPR142 agonists for the treatment of Type II diabetes

  摘要：

  GPR142 is a novel GPCR that is predominantly expressed in pancreatic beta-cells. GPR142 agonists potentiate glucose-dependent insulin secretion, and therefore can reduce the risk of hypoglycemia. Optimization of our lead pyridinone-phenylalanine series led to a proof-of-concept compound 22, which showed in vivo efficacy in mice with dose-dependent increase in insulin secretion and a decrease in glucose levels. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2012.08.015
• 作为产物：
  描述：

  2-Methoxy-5-pyridin-4-ylpyridine-3-carboxamide 以62%的产率得到
  参考文献：
  名称：

  HAGEN, V.;KLAUSCHENZ, E.;PRAGST, F., J. PRAKT. CHEM., 329,(1987) N 5, 793-803

  摘要：

  DOI：
• 作为试剂：
  描述：

  (S)-N-(2-methoxy-5-(pyridin-4-yl)pyridin-3-yl)-3-phenyl-2-(1-(pyridin-2-yl)cyclopropylamino)propanamide 、 2-methoxy-5-(1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazol-5-yl)pyridin-3-amine 在 2-甲氧基-5-(吡啶-4-基)吡啶-3-胺 作用下， 以to give (2S)—N-(2-methoxy-5-(1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazol-5-yl)pyridin-3-yl)-3-phenyl-2-(1-(pyridin-2-yl)cyclopropylamino)propanamide 14.1.D的产率得到(2S)-N-(2-methoxy-5-(1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazol-5-yl)pyridin-3-yl)-3-phenyl-2-(1-(pyridin-2-yl)cyclopropylamino)propanamide
  参考文献：
  名称：

  PHENYLANALINE AMIDE DERIVATIVES USEFUL FOR TREATING INSULIN-RELATED DISEASES AND CONDITIONS

  摘要：

  本文所提供的是I式化合物：其中A、B、X、R1、R2和下标n如下所述。本文还提供了包含该化合物的组合物，以及使用它们的方法，例如用于治疗2型糖尿病和2型糖尿病相关疾病的方法。

  公开号：

  US20120115811A1

文献信息

• Phenylalanine amide derivatives useful for treating insulin-related diseases and conditions
  申请人：Du Xiaohui

  公开号：US08785468B2

  公开（公告）日：2014-07-22

  Provided herein are compounds of formula I: wherein A, B, X, R1, R2 and subscript n are as defined in the following disclosure. Compositions comprising the compounds are also provided, as well as methods for their use, for example, in treatment of type 2 diabetes and type 2 diabetes-related conditions.

  本文提供的是I式化合物，其中A、B、X、R1、R2和下标n的定义如下所述。还提供了包含这些化合物的组合物，以及它们的使用方法，例如用于治疗2型糖尿病和2型糖尿病相关疾病。
• Pyridine derivatives, process for their preparation and composition containing them
  申请人：STERLING DRUG INC.

  公开号：EP0109027A1

  公开（公告）日：1984-05-23

  2-(R,O)-3-Q-5-PY-6-R-pyridine (I) or pharmaceutically acceptable acid-addition salts thereof are useful cardiotonics, where R, is methyl or ethyl, R is hydrogen or lower-alkyl, PY is 4(or 3)-pyridinyl or 4(or 3)-pyridinyl having one or two lower-alkyl substituents, and Q is hydrogen, chloro or COOR' where R' is lower-alkyl, or 0 is cyano only when R is hydrogen. The preparation of I and their cardiotonic use are shown.

  2-(R,O)-3-Q-5-PY-6-R-吡啶（I）或其药学上可接受的酸加成盐是有用的强心剂，其中 R 是甲基或乙基，R 是氢或低级烷基，PY 是 4（或 3）-吡啶基或具有一个或两个低级烷基取代基的 4（或 3）-吡啶基，Q 是氢、氯或 COOR'（其中 R' 是低级烷基），或 0 是氰基（仅当 R 是氢时）。I 的制备方法及其强心剂用途如图所示。
• [EN] PHENYLALANINE AMIDE DERIVATIVES USEFUL FOR TREATING INSULIN-RELATED DISEASES AND CONDITIONS<br/>[FR] DÉRIVÉS DE LA PHÉNYLALANINE-AMIDE UTILES POUR LE TRAITEMENT DE MALADIES ET ÉTATS LIÉS À L'INSULINE
  申请人：AMGEN INC

  公开号：WO2010093849A3

  公开（公告）日：2010-10-28
• Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition
  作者：Daren Fearon、Isaac M. Westwood、Rob L.M. van Montfort、Richard Bayliss、Keith Jones、Vassilios Bavetsias

  DOI：10.1016/j.bmc.2018.04.033

  日期：2018.7

  Screening a 3-aminopyridin-2-one based fragment library against a 26-kinase panel representative of the human kinome identified 3-amino 5 (1-methyl-1H-pyrazol-4-yl)pyridin-2(1H)-one (2) and 3-amino-5(pyridin-4-yl)pyridin-2(1H)-one (3) as ligand efficient inhibitors of the mitotic kinase Monopolar Spindle 1 (MPS1) and the Aurora kinase family. These kinases are well recognised as attractive targets for therapeutic intervention for treating cancer. Elucidation of the binding mode of these fragments and their analogues has been carried out by X-ray crystallography. Structural studies have identified key interactions with a conserved lysine residue and have highlighted potential regions of MPS1 which could be targeted to improve activity and selectivity. (C) 2018 The Authors. Published by Elsevier Ltd.
• Hagen, V.; Klauschenz, E.; Pragst, F., Journal fur praktische Chemie (Leipzig 1954), 1987, vol. 329, # 5, p. 793 - 803
  作者：Hagen, V.、Klauschenz, E.、Pragst, F.

  DOI：——

  日期：——