(R)-1-(2-fluoroethyl)piperidin-3-amine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: (R)-1-(2-fluoroethyl)piperidin-3-amine
• 英文别名: (R)-1-(2-Fluoroethyl)piperidin-3-amine；(3R)-1-(2-fluoroethyl)piperidin-3-amine
• 化学式: C₇H₁₅FN₂
• 分子量: 146.208
• InChiKey: RZCRIYWIMDHDKZ-SSDOTTSWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  29.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (R)-1-(2-fluoroethyl)piperidin-3-amine 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 caesium carbonate 、 N,N-二异丙基乙胺 作用下， 以 1,4-二氧六环 、 水 、 二甲基亚砜 为溶剂， 100.0 ℃ 、101.33 kPa 条件下， 反应 24.0h， 生成 (R)-5-chloro-2-(4-((1-(2-fluoroethyl)piperidin-3-yl)amino)phthalazin-1-yl)phenol
  参考文献：
  名称：

  [EN] FUSED PYRIDAZINE DERIVATIVES AS NLRP3 INHIBITORS
  [FR] DÉRIVÉS DE PYRIDAZINE FUSIONNÉS UTILISÉS COMME INHIBITEURS DE NLRP3

  摘要：

  Disclosed are compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein α, β, m, R5, R6, R7, R9, R10, R11, Ra, Rb, X1, X2, X3, X4and X8are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula (I), to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with NLRP3.

  公开号：

  WO2023194964A1
• 作为产物：
  描述：

  tert-butyl (R)-(1-(2-fluoroethyl)piperidin-3-yl)carbamate 在 盐酸 作用下， 以 1,4-二氧六环 为溶剂， 以98 %的产率得到(R)-1-(2-fluoroethyl)piperidin-3-amine
  参考文献：
  名称：

  [EN] FUSED PYRIDAZINE DERIVATIVES AS NLRP3 INHIBITORS
  [FR] DÉRIVÉS DE PYRIDAZINE FUSIONNÉS UTILISÉS COMME INHIBITEURS DE NLRP3

  摘要：

  Disclosed are compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein α, β, m, R5, R6, R7, R9, R10, R11, Ra, Rb, X1, X2, X3, X4and X8are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula (I), to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with NLRP3.

  公开号：

  WO2023194964A1

文献信息

• [EN] NLRP3 INFLAMMASOME INHIBITORS<br/>[FR] INHIBITEURS D'INFLAMMASOME NLRP3
  申请人：NOVARTIS AG

  公开号：WO2020021447A1

  公开（公告）日：2020-01-30

  The present invention relates to novel thienopyrrolotriazinacetamide compounds of Formula (I): wherein R1, R2 and R3 are defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. The invention further relates to the processes for their preparation, pharmaceutical compositions and medicaments containing them, and their use in the treatment of diseases and disorders mediated by NLRP3.

  本发明涉及一种新型噻吡咯三唑酰胺化合物的化学式（I）：其中R1、R2和R3如本文所定义，该化合物抑制NOD样受体蛋白3（NLRP3）炎症小体活性。该发明还涉及它们的制备过程、含有它们的药物组合物和药物，以及它们在治疗由NLRP3介导的疾病和紊乱中的用途。
• NLRP3 INFLAMMASOME INHIBITORS
  申请人：Novartis AG

  公开号：US20210308140A1

  公开（公告）日：2021-10-07

  The present invention relates to novel thienopyrrolotriazinacetamide compounds of Formula (I): wherein R 1 , R 2 and R 3 are defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. The invention further relates to the processes for their preparation, pharmaceutical compositions and medicaments containing them, and their use in the treatment of disease and disorders mediated by NLRP3.