2-(Trimethylsilyl)ethyl 4-(2-hydroxyethyl)piperidine-1-carboxylate | 628728-11-0

• 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: 2-(Trimethylsilyl)ethyl 4-(2-hydroxyethyl)piperidine-1-carboxylate
• 英文别名: 2-trimethylsilylethyl 4-(2-hydroxyethyl)piperidine-1-carboxylate
• CAS: 628728-11-0
• 化学式: C₁₃H₂₇NO₃Si
• 分子量: 273.448
• InChiKey: YHLSGWLXQQKNIP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.56
• 重原子数：
  18.0
• 可旋转键数：
  5.0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.92
• 拓扑面积：
  49.77
• 氢给体数：
  1.0
• 氢受体数：
  3.0

反应信息

• 作为反应物：
  描述：

  2-(Trimethylsilyl)ethyl 4-(2-hydroxyethyl)piperidine-1-carboxylate 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 生成
  参考文献：
  名称：

  Solid-Phase Polyamine Synthesis Using Piperazine and Piperidine Building Blocks

  摘要：

  Polyamines containing piperidine and piperazine moieties have been synthesized on solid support using S(N)2 alkylation of resin-bound secondary amines with 2-nitrobenzenesulfonates (nosylates). The effect of solvent on this alkylation was investigated. The methodology was employed for the total synthesis of novel analogues of wasp polyamine toxins (philanthotoxins).

  DOI：

  10.1021/ol035610t
• 作为产物：
  描述：

  4-哌啶乙醇 、 对硝基苯基三甲基硅乙基碳酸酯 以 甲醇 、 二氯甲烷 为溶剂， 反应 16.0h， 生成 2-(Trimethylsilyl)ethyl 4-(2-hydroxyethyl)piperidine-1-carboxylate
  参考文献：
  名称：

  Solid-Phase Polyamine Synthesis Using Piperazine and Piperidine Building Blocks

  摘要：

  Polyamines containing piperidine and piperazine moieties have been synthesized on solid support using S(N)2 alkylation of resin-bound secondary amines with 2-nitrobenzenesulfonates (nosylates). The effect of solvent on this alkylation was investigated. The methodology was employed for the total synthesis of novel analogues of wasp polyamine toxins (philanthotoxins).

  DOI：

  10.1021/ol035610t

文献信息

• [EN] COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF KRAS<br/>[FR] COMPOSÉS ET MÉTHODES DE DÉGRADATION CIBLÉE DE KRAS
  申请人：ARVINAS OPERATIONS INC

  公开号：WO2023141570A2

  公开（公告）日：2023-07-27

  Bifunctional compounds, which find utility as modulators of Kirsten ras sarcoma protein (KRAS), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the Von Hippel-Lindau E3 ubiquitin ligase and on the other end a moiety which binds KRAS, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-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 aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

  本文描述了可用作 Kirsten RAs 肉瘤蛋白（KRAS）调节剂的双功能化合物。特别是，本公开的杂双官能化合物一端含有与 Von Hippel-Lindau E3 泛素连接酶结合的分子，另一端含有与 KRAS 结合的分子，从而将靶蛋白置于泛素连接酶附近，以实现对靶蛋白的降解（和抑制）。本公开的杂双官能团化合物具有与降解/抑制靶蛋白相关的多种药理活性。本发明公开的化合物和组合物可以治疗或预防由于靶蛋白调节失常而导致的疾病或失调。