(R)-(+)-4-phenyl-2-oxazolidinone lithium salt

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑烷类
• 英文名称: (R)-(+)-4-phenyl-2-oxazolidinone lithium salt
• 英文别名: lithium;(4R)-4-phenyl-4,5-dihydro-1,3-oxazol-2-olate
• 化学式: C₉H₈NO₂*Li
• 分子量: 169.109
• InChiKey: HRFWPCNUKHEZCG-QRPNPIFTSA-M

计算性质

• 辛醇/水分配系数(LogP)：
  -0.74
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  27.3
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (R)-(+)-4-phenyl-2-oxazolidinone lithium salt 在 N-溴代丁二酰亚胺(NBS) 、 三氟甲磺酸二丁硼 、 三甲基乙酰氯 、 三乙胺 、 N,N-二异丙基乙胺 作用下， 生成 (4R)-3-[(2R,3R)-2-bromo-4-methyl-3-phenylpentanoyl]-4-phenyl-1,3-oxazolidin-2-one
  参考文献：
  名称：

  光学纯β-异丙基苯基丙氨酸的不对称合成：一种新的β-支链异常氨基酸

  摘要：

  高度构象受限的不寻常氨基酸β-异丙基苯基丙氨酸的所有四个光学纯异构体均已不对称合成。

  DOI：

  10.1016/0040-4039(96)00091-3
• 作为产物：
  描述：

  (R)-4-苯基-2-唑烷酮 在 正丁基锂 作用下， 以 四氢呋喃 为溶剂， 反应 0.5h， 生成 (R)-(+)-4-phenyl-2-oxazolidinone lithium salt
  参考文献：
  名称：

  设计和合成全局受限的Grb2 SH2域抑制剂的烯烃复分解。

  摘要：

  经常与烯烃复分解介导的肽大环化有关的一个缺点，即在闭环位点的侧链官能度的丧失，可以通过在闭环烯烃链段内掺入侧链官能度来避免。这种方法在大环Grb2 SH2域拮抗剂的制备中得到了证明，该拮抗剂设计为构象约束的β弯曲模拟物。

  DOI：

  10.1021/ol0157609

文献信息

• Macrocyclic inhibitors of the PD-1/PD-L1 and CD80(B7-1)/PD-L1 protein/protein interactions
  申请人：Bristol-Myers Squibb Company

  公开号：US09308236B2

  公开（公告）日：2016-04-12

  The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.

  本公开提供了一种新型的大环肽，可以抑制PD-1/PD-L1和PD-L1/CD80蛋白质相互作用，因此对改善包括癌症和传染病在内的各种疾病有用。
• [EN] PHENYLALANINE DERIVATIVES AS DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES<br/>[FR] DERIVES DE PHENYLALANINE UTILISES COMME INHIBITEURS DE LA DIPEPTIDYL PEPTIDASE DANS LE TRAITEMENT OU LA PREVENTION DU DIABETE
  申请人：MERCK & CO INC

  公开号：WO2004043940A1

  公开（公告）日：2004-05-27

  The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

  本发明涉及苯丙氨酸衍生物，这些衍生物是二肽基肽酶-IV酶（'DP-IV抑制剂'）的抑制剂，并且在治疗或预防涉及二肽基肽酶-IV酶的疾病中具有用处，如糖尿病，特别是2型糖尿病。该发明还涉及包含这些化合物的药物组合物以及在预防或治疗涉及二肽基肽酶-IV酶的这类疾病中使用这些化合物和组合物。
• [EN] CYCLOHEXYLALANINE DERIVATIVES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES<br/>[FR] DERIVES DE LA CYCLOHEXYLALANINE UTILISES COMME INHIBITEURS DE LA DIPEPTIDYL PEPTIDASE-IV POUR LE TRAITEMENT OU LA PREVENTION DES DIABETES
  申请人：MERCK & CO INC

  公开号：WO2005116029A1

  公开（公告）日：2005-12-08

  The present invention is directed to novel cyclohexylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

  本发明涉及新颖的环己基丙氨酸衍生物，这些衍生物是二肽基肽酶-IV酶（'DP-IV抑制剂'）的抑制剂，并且在治疗或预防涉及二肽基肽酶-IV酶的疾病中具有用处，如糖尿病，特别是2型糖尿病。该发明还涉及包含这些化合物的药物组合物，以及在预防或治疗涉及二肽基肽酶-IV酶的这类疾病中使用这些化合物和组合物。
• Thiazole compounds and methods of use
  申请人：Zeng Qingping

  公开号：US20070173506A1

  公开（公告）日：2007-07-26

  The invention relates to thiazole compounds of Formula I and Formula II and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

  该发明涉及Formula I和Formula II的噻唑化合物及其组合物，用于治疗由蛋白激酶B（PKB）介导的疾病，其中变量具有此处提供的定义。该发明还涉及这种噻唑化合物及其组合物在治疗与异常细胞生长、癌症、炎症和代谢紊乱相关的疾病状态中的治疗用途。
• Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use
  申请人：Burke, Jr. Terrence R.

  公开号：US10266565B2

  公开（公告）日：2019-04-23

  Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.

  提供了一种新型化合物，通过波洛盒结构结合波洛样激酶。在某些实施例中，这些新型化合物是PEG化肽。根据本发明，这些PEG化肽表现出高PBD结合亲和力。在某些实施例中，这些PEG化肽在整个细胞系统中也表现出活性。本发明还提供了一种通过波洛盒结构结合波洛样激酶且具有降低阴离子电荷的化合物。此外，还提供了PEG化肽的设计和/或合成方法以及使用这些方法。本发明提供了这些化合物的使用方法和合成方法。