(2R)-1-(6-chloro-5-methylpyridin-3-yl)oxy-N-methylpropan-2-amine

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (2R)-1-(6-chloro-5-methylpyridin-3-yl)oxy-N-methylpropan-2-amine
• 化学式: C₁₀H₁₅ClN₂O
• 分子量: 214.695
• InChiKey: WLKGRSYKSXOUEF-MRVPVSSYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  34.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  5-[(R)-2-N-BOC-amino-1-propyloxy]-2-chloro-3-bromo pyridine 在 nickel(II) iodide 、 sodium hydride 作用下， 生成 (2R)-1-(6-chloro-5-methylpyridin-3-yl)oxy-N-methylpropan-2-amine
  参考文献：
  名称：

  Synthesis and biological evaluation of pyridine-modified analogues of 3-(2-Aminoethoxy)pyridine as novel nicotinic receptor ligands

  摘要：

  Analogues of the potent nicotinic receptor agonist 3-(2-aminoethoxy)pyridine substituted at the 5' and 6'-positions of the pyridine ring were synthesized and tested in vitro for nicotinic receptor binding activity (displacement of [H-3](-)cytisine from whole rat brain synaptic membranes). The substituted analogues exhibited K-i values ranging from 0.076 to 319 nM compared to a K-i value of 26 nM for compound 1. Among the compounds tested, 5'-vinyl-6'-chloro substituted I was the most potent. (C) 2002 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(02)00740-0

文献信息

• SUBSTITUTED PYRIDINE COMPOUNDS USEFUL FOR CONTROLLING CHEMICAL SYNAPTIC TRANSMISSION
  申请人：ABBOTT LABORATORIES

  公开号：EP1257535A1

  公开（公告）日：2002-11-20
• [EN] SUBSTITUTED PYRIDINE COMPOUNDS USEFUL FOR CONTROLLING CHEMICAL SYNAPTIC TRANSMISSION<br/>[FR] COMPOSES PYRIDINE SUBSTITUES UTILES DANS LA REGULATION DE LA TRANSMISSION SYNAPTIQUE CHIMIQUE
  申请人：ABBOTT LAB

  公开号：WO2001056991A1

  公开（公告）日：2001-08-09

  The present invention is directed to a series of substituted pyridine compounds (I), a method for selectively controlling neurotransmitter release in mammals using these compounds, and pharmaceutical compositions containing these compounds. Preferred compounds are 3'-(5'- and/or 6'-substituted) pyridyl ethers. n = 1-4, R1-R6 as in the claims.
• Synthesis and biological evaluation of pyridine-modified analogues of 3-(2-Aminoethoxy)pyridine as novel nicotinic receptor ligands
  作者：Nan-Horng Lin、Liming Dong、William H Bunnelle、David J Anderson、Michael D Meyer

  DOI：10.1016/s0960-894x(02)00740-0

  日期：2002.11

  Analogues of the potent nicotinic receptor agonist 3-(2-aminoethoxy)pyridine substituted at the 5' and 6'-positions of the pyridine ring were synthesized and tested in vitro for nicotinic receptor binding activity (displacement of [H-3](-)cytisine from whole rat brain synaptic membranes). The substituted analogues exhibited K-i values ranging from 0.076 to 319 nM compared to a K-i value of 26 nM for compound 1. Among the compounds tested, 5'-vinyl-6'-chloro substituted I was the most potent. (C) 2002 Elsevier Science Ltd. All rights reserved.