tert-butyl (2S,4R)-4-hydroxy-2-((trityloxy)methyl)pyrrolidine-1-carboxylate | 1315590-89-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: tert-butyl (2S,4R)-4-hydroxy-2-((trityloxy)methyl)pyrrolidine-1-carboxylate
• 英文别名: (2S,4R)-tert-butyl 4-hydroxy-2-(trityloxymethyl)pyrrolidine-1-carboxylate；(2S,4R)-tert-Butyl 4-hydroxy-2-((trityloxy)methyl)pyrrolidine-1-carboxylate；tert-butyl (2S,4R)-4-hydroxy-2-(trityloxymethyl)pyrrolidine-1-carboxylate
• CAS: 1315590-89-6
• 化学式: C₂₉H₃₃NO₄
• 分子量: 459.585
• InChiKey: XMJRQZWPOQOBPC-IZZNHLLZSA-N

物化性质

• 沸点：
  566.9±50.0 °C(Predicted)
• 密度：
  1.161±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  34
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.34
• 拓扑面积：
  59
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  tert-butyl (2S,4R)-4-hydroxy-2-((trityloxy)methyl)pyrrolidine-1-carboxylate 在 三乙胺 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 0.5h， 生成 tert-butyl (2S,4R)-4-(4-fluorophenoxy)-2-(trityloxymethyl)pyrrolidine-1-carboxylate
  参考文献：
  名称：

  Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors

  摘要：

  The synthesis and SAR for a novel series of pyrrolotriazines as pan-Aurora kinase inhibitors are described. Optimization of the cyclopropane carboxamide terminus of lead compound 1 resulted in analogs with high cellular activity and improved rat PK profiles. Notably, compound 17l demonstrated tumor growth inhibition in a mouse xenograft model. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.07.027
• 作为产物：
  描述：

  N-Boc-反式-4-羟基-L-脯氨酸甲酯 在 吡啶 、 锂硼氢 作用下， 以 四氢呋喃 为溶剂， 反应 101.0h， 生成 tert-butyl (2S,4R)-4-hydroxy-2-((trityloxy)methyl)pyrrolidine-1-carboxylate
  参考文献：
  名称：

  Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors

  摘要：

  The synthesis and SAR for a novel series of pyrrolotriazines as pan-Aurora kinase inhibitors are described. Optimization of the cyclopropane carboxamide terminus of lead compound 1 resulted in analogs with high cellular activity and improved rat PK profiles. Notably, compound 17l demonstrated tumor growth inhibition in a mouse xenograft model. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.07.027

文献信息

• [EN] AURORA KINASE COMPOUNDS AND METHODS OF THEIR USE<br/>[FR] COMPOSÉS DE KINASE AURORA ET LEURS MÉTHODES D'UTILISATION
  申请人：AMBIT BIOSCIENCES CORP

  公开号：WO2011088045A1

  公开（公告）日：2011-07-21

  Provided herein are pyrrolotriazine compounds for treatment of Aurora kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.

  本文提供了用于治疗由Aurora激酶介导的疾病的吡咯三嗪化合物。还提供了包含这些化合物的药物组合物以及使用这些化合物和组合物的方法。
• PEGYLATED LIPID COMPOUNDS AND METHODS OF USE THEREOF
  申请人：[en]RENAGADE THERAPEUTICS MANAGEMENT INC.

  公开号：WO2024044728A1

  公开（公告）日：2024-02-29

  The present disclosure relates to PEGylated lipid compounds and pharmaceutically acceptable salts thereof. Such compounds are useful, for example, as constituent parts of lipid nanoparticle (LNP) formulations for delivery of various active agents. The present disclosure further provides LNPs comprising a disclosed compound. Also provided herein are methods of preparing such PEGylated lipid compounds, as well as pharmaceutical compositions comprising an LNP and an active agent; and methods of use thereof.