(2,5-Dioxopyrrolidin-1-yl) 2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetate | 1196075-64-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酰胺类
• 英文名称: (2,5-Dioxopyrrolidin-1-yl) 2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetate
• 英文别名: (2,5-dioxopyrrolidin-1-yl) 2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetate
• CAS: 1196075-64-5
• 化学式: C₂₀H₂₁N₃O₈
• 分子量: 431.402
• InChiKey: FPMPPQVILQNDSS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.8
• 重原子数：
  31
• 可旋转键数：
  10
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  139
• 氢给体数：
  1
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  (2,5-Dioxopyrrolidin-1-yl) 2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetate 生成 4-[4-[3-Oxo-3-(2-oxoazetidin-1-yl)propyl]phenyl]morpholine-3,5-dione
  参考文献：
  名称：

  PROCESSES FOR PREPARING PEPTIDE CONJUGATES AND LINKERS

  摘要：

  本发明提供了一种制备5b式化合物的方法，以及其中间体，以及用于制备这些类似化合物的新型化合物类。

  公开号：

  US20150031108A1
• 作为产物：
  描述：

  3-(4-硝基苯基)丙酸 在 盐酸 、 正丁基锂 、 氯化亚砜 、 palladium 10% on activated carbon 、 氢气 、 N,N'-二异丙基碳二亚胺 作用下， 以 四氢呋喃 为溶剂， -70.0~25.0 ℃ 、170.28 kPa 条件下， 反应 19.25h， 生成 (2,5-Dioxopyrrolidin-1-yl) 2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetate
  参考文献：
  名称：

  Chromatography- and Lyophilization-Free Synthesis of a Peptide-Linker Conjugate

  摘要：

  An optimized and scalable process to manufacture peptide-linker conjugate 1 is reported that avoids the chromatographic purification and lyophilization that are typically required for the isolation of this type of compound. An operationally simple protocol has been developed that couples the peptide to the linker in DMF followed by precipitation with MeCN. A scalable synthesis of the linker is also described which features the N-acylation of 2-azetidinone promoted by 1-propanephosphonic acid anhydride (T3P). The number of operations during the second step of the synthesis (nitrobenzene reduction to aniline) has been simplified by telescoping the aniline into the next step (reaction with diglycolic anhydride to form an acid), thus avoiding an additional isolation. Finally, two efficient activation methods for the acid have been developed by means of the corresponding pentafluorophenyl (PFP) and p-nitrophenyl (PNP) esters.

  DOI：

  10.1021/op4002998

文献信息

• PROCESSES FOR PREPARING PEPTIDE CONJUGATES AND LINKERS
  申请人：PFIZER INC.

  公开号：US20150031108A1

  公开（公告）日：2015-01-29

  The present invention provides a process for preparing a compound of Formula 5b, as well as intermediates thereof, and novel classes of compounds useful in process for preparing these and similar compounds.

  本发明提供了一种制备5b式化合物的方法，以及其中间体，以及用于制备这些类似化合物的新型化合物类。
• PROCESS FOR PURIFYING A SAMPLE OF H38C2 ANTIBODY
  申请人：Pfizer Inc.

  公开号：EP2793928B1

  公开（公告）日：2017-03-15
• ANTI-ANGIOGENIC COMPOUNDS
  申请人：Doppalapudi Venkata Ramana

  公开号：US20100003267A1

  公开（公告）日：2010-01-07

  The present invention provides VEGF binding peptides. In addition, the invention provides VEGF peptides conjugated to antibodies alone and in conjunction with other anti-angiogenic molecules. Various uses of the peptides and compounds are provided, including methods to treat disorders associated with abnormal angiogenesis.
• Anti-Diabetic Compounds
  申请人：Das Tapan Kanti

  公开号：US20120282279A1

  公开（公告）日：2012-11-08

  The present invention provides a FGF21 molecule covalently attached to the combining site of an antibody via a linker, wherein the linker is covalently attached to the side chain of a linking residue within FGF21. Various uses of the compounds are provided, including methods to prevent or treat diabetes or diabetes-related conditions.
• ANTI-DIABETIC COMPOUNDS
  申请人：PFIZER INC.

  公开号：US20130164310A1

  公开（公告）日：2013-06-27

  The present invention provides a composition of the formula: [FGF21-1 st Linker]-[Ab]-[2 nd -Linker-Ex4]; wherein FGF21 is an FGF21 homologue; and Ex4 is an Exendin4 homologue; and Ab is an aldolase catalytic antibody or antigen binding portion thereof; and the 1 st linker is covalently attached to the side chain of a protein-linking residue in FGF21 and to a combining site of the antibody, and the 2 nd linker is covalently attached to the side chain of a peptide-linking residue in Ex4 and to a combining site of the antibody, and wherein the first and second linker are the same or different. Various uses of the compounds are provided, including methods to prevent or treat diabetes or diabetes-related conditions.