N-[(1S)-1-(5-fluoropyridin-2-yl)ethyl]-N-(5-methyl-1-pyrazol-3-yl)pyrazine-2,6-diamine | 1065267-55-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: N-[(1S)-1-(5-fluoropyridin-2-yl)ethyl]-N-(5-methyl-1-pyrazol-3-yl)pyrazine-2,6-diamine
• 英文别名: (S)-N2-(1-(5-fluoropyridin-2-yl)ethyl)-N6-(5-methyl-1H-pyrazol-3-yl)pyrazine-2,6-diamine；2-N-[(1S)-1-(5-fluoropyridin-2-yl)ethyl]-6-N-(5-methyl-1H-pyrazol-3-yl)pyrazine-2,6-diamine
• CAS: 1065267-55-1
• 化学式: C₁₅H₁₆FN₇
• 分子量: 313.337
• InChiKey: KTPAQUKUOMIFDN-JTQLQIEISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  23
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  91.4
• 氢给体数：
  3
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  6-chloro-N-[(1S)-1-(5-fluoropyridin-2-yl)ethyl]pyrazin-2-amine 、 2-甲基-2-丙基3-氨基-5-甲基-1H-吡唑-1-羧酸酯 在 tris-(dibenzylideneacetone)dipalladium(0) 、 caesium carbonate 、 4,5-双二苯基膦-9,9-二甲基氧杂蒽 作用下， 以 1,4-二氧六环 为溶剂， 生成 N-[(1S)-1-(5-fluoropyridin-2-yl)ethyl]-N-(5-methyl-1-pyrazol-3-yl)pyrazine-2,6-diamine
  参考文献：
  名称：

  Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors

  摘要：

  The design, synthesis and biological evaluation of a series of pyrazol-3-ylamino pyrazines as potent and selective JAK2 kinase inhibitors is reported, along with the pharmacokinetic and pharmacodynamic properties of lead compounds. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.10.054

文献信息

• [EN] PYRAZOLYL-AMINO-SUBSTITUTED PYRAZINES AND THEIR USE FOR THE TREATMENT OF CANCER<br/>[FR] PYRAZINES PYRAZOLYL-AMINO SUBSTITUÉES ET UTILISATION DE CES COMPOSÉS POUR LE TRAITEMENT DU CANCER
  申请人：ASTRAZENECA AB

  公开号：WO2008117050A1

  公开（公告）日：2008-10-02

  [EN] The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These novel compounds provide a treatment for myeloproliferative disorders and cancer.
  [FR] La présente invention concerne des composés de formule (I); leurs compositions pharmaceutiques, et leurs procédés d'utilisation. Ces nouveaux composés fournissent un traitement pour les troubles myéloprolifératifs et le cancer.
• Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors
  作者：Stephanos Ioannidis、Michelle L. Lamb、Audrey M. Davies、Lynsie Almeida、Mei Su、Geraldine Bebernitz、Minwei Ye、Kirsten Bell、Marat Alimzhanov、Michael Zinda

  DOI：10.1016/j.bmcl.2009.10.054

  日期：2009.12

  The design, synthesis and biological evaluation of a series of pyrazol-3-ylamino pyrazines as potent and selective JAK2 kinase inhibitors is reported, along with the pharmacokinetic and pharmacodynamic properties of lead compounds. (C) 2009 Elsevier Ltd. All rights reserved.