2-苄基-1-氧代-2,8-二氮杂螺[4.5]癸烷-8-羧酸叔丁酯 | 155600-89-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: 2-苄基-1-氧代-2,8-二氮杂螺[4.5]癸烷-8-羧酸叔丁酯
• 中文别名: 2-苄基-1-氧代-2,7-二氮杂螺[3.5]壬烷-7-羧酸叔丁酯
• 英文名称: tert-Butyl 2-benzyl-1-oxo-2,7-diazaspiro[3.5]nonane-7-carboxylate
• 英文别名: tert-butyl 2-benzyl-3-oxo-2,7-diazaspiro[3.5]nonane-7-carboxylate
• CAS: 155600-89-8
• 化学式: C₁₉H₂₆N₂O₃
• 分子量: 330.427
• InChiKey: GGDGRVBFSAZNLK-UHFFFAOYSA-N

物化性质

• 沸点：
  497.3±45.0 °C(Predicted)
• 密度：
  1.18±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  24
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.58
• 拓扑面积：
  49.8
• 氢给体数：
  0
• 氢受体数：
  3

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  2-苄基-1-氧代-2,8-二氮杂螺[4.5]癸烷-8-羧酸叔丁酯 在 苯甲醚 、 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 0.25h， 以80%的产率得到2-苄基-2,7-二氮杂螺[3.5]壬烷-3-酮
  参考文献：
  名称：

  Synthesis of a new series of 2,7-diazaspiro[3.5]nonan-1-ones and study of their cholinergic properties

  摘要：

  A new series of substituted 2,7-diazaspiro[3.5]nonan-1-ones (la-1), structurally related to the muscarinic agonist RS-86, has been synthesized and tested for cholinergic properties both in vitro and in vivo. None of the compounds showed significant cholinergic properties at either the central or peripheral level. A possible explanation for the lack of activity is given.

  DOI：

  10.1016/0223-5234(94)90207-0
• 作为产物：
  描述：

  二碳酸二叔丁酯 在 lithium diisopropyl amide 作用下， 以 氯仿 为溶剂， 反应 22.0h， 生成 2-苄基-1-氧代-2,8-二氮杂螺[4.5]癸烷-8-羧酸叔丁酯
  参考文献：
  名称：

  Synthesis of a new series of 2,7-diazaspiro[3.5]nonan-1-ones and study of their cholinergic properties

  摘要：

  A new series of substituted 2,7-diazaspiro[3.5]nonan-1-ones (la-1), structurally related to the muscarinic agonist RS-86, has been synthesized and tested for cholinergic properties both in vitro and in vivo. None of the compounds showed significant cholinergic properties at either the central or peripheral level. A possible explanation for the lack of activity is given.

  DOI：

  10.1016/0223-5234(94)90207-0

文献信息

• [EN] MODULATORS OF BCL6 PROTEOLYSIS AND ASSOCIATED METHODS OF USE<br/>[FR] MODULATEURS DE PROTÉOLYSE BCL6 ET PROCÉDÉS D'UTILISATION ASSOCIÉS
  申请人：ARVINAS OPERATIONS INC

  公开号：WO2022221673A1

  公开（公告）日：2022-10-20

  Bifunctional compounds, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a cereblon ligand that binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

  本文描述了双功能化合物，其作为B细胞淋巴瘤6蛋白（BCL6；目标蛋白）调节剂而发挥作用。具体而言，本公开的双功能化合物在一端含有结合到各自E3泛素连接酶的小脑球蛋白配体，而在另一端含有结合到目标蛋白的基团，从而将目标蛋白置于泛素连接酶的近旁，以实现目标蛋白的降解（和抑制）。本公开的双功能化合物表现出与目标蛋白的降解/抑制相关的广泛的药理活性。使用本公开的化合物和组合物治疗或预防由目标蛋白的聚集或积累引起的疾病或障碍。
• MODULATORS OF BCL6 PROTEOLYSIS AND ASSOCIATED METHODS OF USE
  申请人：Arvinas Operations, Inc.

  公开号：US20220395576A1

  公开（公告）日：2022-12-15

  Bifunctional compounds, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a cereblon ligand that binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.