5-[(R)-2-N-BOC-amino-1-propyloxy]-2-fluoro pyridine | 352705-09-0

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 5-[(R)-2-N-BOC-amino-1-propyloxy]-2-fluoro pyridine
• 英文别名: tert-butyl N-[(2R)-1-(6-fluoropyridin-3-yl)oxypropan-2-yl]carbamate
• CAS: 352705-09-0
• 化学式: C₁₃H₁₉FN₂O₃
• 分子量: 270.304
• InChiKey: ZSTHKGZHAPPXII-SECBINFHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  19
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  60.4
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  5-[(R)-2-N-BOC-amino-1-propyloxy]-2-fluoro pyridine 在 sodium hydroxide 、 聚合甲醛 、 甲酸 作用下， 以 水 为溶剂， 以53%的产率得到5-[(R)-2-dimethylamino-1-propyloxy]-2-fluoro pyridine
  参考文献：
  名称：

  Substituted pyridine compounds useful for controlling chemical synaptic transmission

  摘要：

  本发明涉及一系列替代吡啶化合物，以及使用这些化合物在哺乳动物中选择性控制神经递质释放的方法和含有这些化合物的药物组合物。首选化合物是3'-(5'和/或6'-取代)吡啶醚。

  公开号：

  US20020058646A1
• 作为产物：
  描述：

  2-氟-5-羟基吡啶 、 alkaline earth salt of/the/ methylsulfuric acid 生成 5-[(R)-2-N-BOC-amino-1-propyloxy]-2-fluoro pyridine
  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
• US6656958B2
  申请人：——

  公开号：US6656958B2

  公开（公告）日：2003-12-02
• [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.
• Substituted pyridine compounds useful for controlling chemical synaptic transmission
  申请人：——

  公开号：US20010034357A1

  公开（公告）日：2001-10-25

  The present invention is directed to a series of substituted pyridine compounds, 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.

  本发明涉及一系列取代吡啶化合物，一种利用这些化合物在哺乳动物中选择性控制神经递质释放的方法，以及含有这些化合物的药物组合物。首选的化合物是3′-(5′-和/或6′-取代)吡啶醚。