(2S,4R)-2-Allyloxycarbonyl-4-hydroxy-pyrrolidine | 220993-21-5

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: (2S,4R)-2-Allyloxycarbonyl-4-hydroxy-pyrrolidine
• 英文别名: trans-4-Hydroxy-l-proline allyl ester；prop-2-enyl (2S,4R)-4-hydroxypyrrolidine-2-carboxylate
• CAS: 220993-21-5
• 化学式: C₈H₁₃NO₃
• 分子量: 171.196
• InChiKey: MXBBYJRDPCRTFD-RQJHMYQMSA-N

物化性质

• 沸点：
  291.6±40.0 °C(Predicted)
• 密度：
  1.160±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  12
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  58.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  4-hydroxyproline 在 p-TSA 作用下， 以 甲苯 为溶剂， 以91%的产率得到(2S,4R)-2-Allyloxycarbonyl-4-hydroxy-pyrrolidine
  参考文献：
  名称：

  Antibiotic oxazolidinone derivatives

  摘要：

  这项发明涉及以下式(I)的化合物：其中，例如：T的式为(IA)、(IB)或(IC)；R1的式为—NHC(═O)Rb，其中Rb为(1-4C)烷基；R2和R3为氢或氟；>A—B—为>C═CH—（但当T为(IA)时除外）或>CH—CH2—；其中当T为(IA)或(IB)的式时；R6为，例如，(1-4C)烷基；R5为氢、R10CO—、R10SO2—或R10CS—，其中R10为，例如，可选择地取代的苯基，或(1-10C)烷基，或当T为(IA)、(IB)或(IC)的式时：R5和R6相连形成与(IA)、(IB)或(IC)中所示环融合的5-或6-成员环，从而形成可选择地取代的双环环，并且其药学上可接受的盐，其制备方法，含有它们的药物组合物，以及它们作为抗菌剂的用途。

  公开号：

  US06605630B1

文献信息

• Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an E3 ubiquitin ligase
  申请人：YALE UNIVERSITY

  公开号：US10730862B2

  公开（公告）日：2020-08-04

  The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides.

  本发明涉及双功能化合物，它们可作为靶向泛素化的调节剂，特别是本发明双功能化合物降解和/或以其他方式抑制的各种多肽和其他蛋白质的抑制剂。特别是，本发明涉及的化合物一端含有与泛素连接酶结合的 VHL 配体，另一端含有与靶蛋白结合的分子，从而使靶蛋白靠近泛素连接酶，以达到降解（和抑制）该蛋白的效果。本发明显示了与本发明化合物相关的广泛药理活性，与降解/抑制靶向多肽的作用相一致。
• GLYCYRRHETINIMIDYL HYDROXYPROLINE ALKYL ESTERS AND PROTECTED DERIVATIVES THEREOF
  申请人：Revlon Consumer Products Corporation

  公开号：EP2961480B1

  公开（公告）日：2017-11-01
• Compounds & Methods for the Enhanced Degradation of Targeted Proteins & Other Polypeptides by an E3 Ubiquitin Ligase
  申请人：YALE UNIVERSITY

  公开号：US20190127359A1

  公开（公告）日：2019-05-02

  The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.
• US6605630B1
  申请人：——

  公开号：US6605630B1

  公开（公告）日：2003-08-12
• US9439845B2
  申请人：——

  公开号：US9439845B2

  公开（公告）日：2016-09-13