tert-butyl [4-(2-hydroxyethyl)pyridin-3-yl]carbamate | 486422-87-1

• 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
• 英文名称: tert-butyl [4-(2-hydroxyethyl)pyridin-3-yl]carbamate
• 英文别名: tert-Butyl 4-(2-hydroxyethyl)pyridin-3-ylcarbamate；tert-butyl N-[4-(2-hydroxyethyl)pyridin-3-yl]carbamate
• CAS: 486422-87-1
• 化学式: C₁₂H₁₈N₂O₃
• 分子量: 238.287
• InChiKey: CIRKCHZDOPHNRA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  17
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  71.4
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  tert-butyl [4-(2-hydroxyethyl)pyridin-3-yl]carbamate 在 盐酸 、 sodium hydroxide 作用下， 以 水 为溶剂， 反应 48.0h， 以26%的产率得到2,3-二氢-1H-吡咯并[2,3-C]吡啶
  参考文献：
  名称：

  Preparation of azaindolines and benzoyl substituted azaindolines: precursors of triazabenzo[cd]azulen-9-one PDE4 inhibitors

  摘要：

  The syntheses of various substituted azaindolines are described. Azaindolines were identified as potential key intermediates towards new PDE4 inhibitors. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2011.08.009
• 作为产物：
  描述：

  3-硝基-4-吡啶乙酸乙酯 在 palladium 10% on activated carbon 、 氢气 、 二异丁基氢化铝 、 三乙胺 作用下， 以 四氢呋喃 、 乙醇 、 二氯甲烷 为溶剂， 20.0 ℃ 、300.01 kPa 条件下， 反应 20.0h， 生成 tert-butyl [4-(2-hydroxyethyl)pyridin-3-yl]carbamate
  参考文献：
  名称：

  Preparation of azaindolines and benzoyl substituted azaindolines: precursors of triazabenzo[cd]azulen-9-one PDE4 inhibitors

  摘要：

  The syntheses of various substituted azaindolines are described. Azaindolines were identified as potential key intermediates towards new PDE4 inhibitors. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2011.08.009

文献信息

• Arylamines for the treatment of conditions associated with gsk-3
  申请人：Berg Stefan

  公开号：US20060052396A1

  公开（公告）日：2006-03-09

  The present invention relates to new compounds of formula (I) wherein Z, Y, X, P, Q, R, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , A, m and n are defined as in any one of claims 1 to 3, a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds for the treatment of conditions associated with glycogens synthase kinase-3 (GSK3).

  本发明涉及具有公式（I）的新化合物，其中Z、Y、X、P、Q、R、R1、R2、R3、R4、R5、R6、R7、R8、R9、R10、R11、R12、A、m和n的定义如权利要求1至3中的任意一项，以及制备它们的过程和其中制备的新中间体，含有所述治疗活性化合物的制药配方以及使用所述活性化合物治疗与糖原合酶激酶-3（GSK3）相关的疾病的方法。
• Heterocyclic amines for the treatment of conditions associated with gsk-3
  申请人：——

  公开号：US20040186113A1

  公开（公告）日：2004-09-23

  The present invention relates to new compounds of the formula (I) wherein Y, X, P, Q, R 1 , R 2 , R 3 , R 4 , R 5A , R 6 , R 7 , R 8 , R 9 , A, B, n, m are defined as in claim 1, a process for their preparation, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds for the treatment of conditions associated with glycogen synthase kinase-3 (GSK3) as well as an intermediate used in the preparation of said compounds. 1

  本发明涉及公式（I）的新化合物，其中Y，X，P，Q，R1，R2，R3，R4，R5A，R6，R7，R8，R9，A，B，n，m的定义如权利要求书中所述，以及其制备过程，含有所述治疗活性化合物的制药配方以及所述活性化合物用于治疗与糖原合成酶激酶-3（GSK3）相关的疾病的用途，以及用于制备所述化合物的中间体。
• Preparation of azaindolines and benzoyl substituted azaindolines: precursors of triazabenzo[cd]azulen-9-one PDE4 inhibitors
  作者：Matthew Badland、Ingrid Devillers、Corinne Durand、Véronique Fasquelle、Bernard Gaudillière、Henry Jacobelli、Ajith C. Manage、Isabelle Pevet、Jocelyne Puaud、Anthony J. Shorter、Roger Wrigglesworth

  DOI：10.1016/j.tetlet.2011.08.009

  日期：2011.10

  The syntheses of various substituted azaindolines are described. Azaindolines were identified as potential key intermediates towards new PDE4 inhibitors. (C) 2011 Elsevier Ltd. All rights reserved.