N-isopropyl-3,4-dibromomaleimide | 717882-15-0

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: N-isopropyl-3,4-dibromomaleimide
• 英文别名: 3,4-Dibromo-1-propan-2-ylpyrrole-2,5-dione；3,4-dibromo-1-propan-2-ylpyrrole-2,5-dione
• CAS: 717882-15-0
• 化学式: C₇H₇Br₂NO₂
• 分子量: 296.946
• InChiKey: QOYHNDOCXZNBLQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  37.4
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  甲基3,4-二溴-2,5-二氧代-2H-吡咯-1(5H)-羧酸叔丁酯 、 异丙胺 以 二氯甲烷 为溶剂， 反应 6.0h， 以60%的产率得到N-isopropyl-3,4-dibromomaleimide
  参考文献：
  名称：

  A mild synthesis of N-functionalised bromomaleimides, thiomaleimides and bromopyridazinediones

  摘要：

  Bromomaleimides are useful building blocks in synthesis and powerful reagents for the selective chemical modification of proteins. A mild new synthesis of these reagents is described, along with the convenient transferability of the approach to dithiomaleimides and bromopyridazinediones. (c) 2013 The Authors. Published by Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2013.04.088

文献信息

• CD30 TARGETING ANTIBODY DRUG CONJUGATES AND USES THEREOF
  申请人：Ludwig-Maximilians-Universitaet Muenchen

  公开号：US20220193251A1

  公开（公告）日：2022-06-23

  The present invention relates to an antibody-drug conjugate (ADC) comprising: (a) Brentuximab, wherein Brentuximab comprises at the C-terminus of the light chains, the heavy chains or all of the heavy and light chains of the Brentuximab a recognition sequence for tubulin tyrosine ligase and a non-natural amino acid; and (b) at least one drug moiety; wherein a drug moiety is coupled to each of the non-natural amino acids via a linker. The present invention further relates to methods of producing same, pharmaceutical compositions comprising same as well as uses thereof.

  本发明涉及一种抗体药物偶联物（ADC），包括：（a）Brentuximab，其中Brentuximab在轻链、重链或所有重链和轻链的C-末端具有识别微管蛋白酪氨酸连接酶的识别序列和非天然氨基酸；以及（b）至少一种药物基团；其中每个药物基团通过连接剂连接到每个非天然氨基酸上。本发明还涉及制备该ADC的方法、包含该ADC的制药组合物以及其用途。
• [EN] STEROID CONJUGATE<br/>[FR] CONJUGUÉ DE STÉROÏDES<br/>[ZH] 一种甾体偶联物
  申请人：[en]DUALITY BIOLOGICS (SUZHOU) CO., LTD.;[zh]映恩生物制药（苏州）有限公司

  公开号：WO2022135332A1

  公开（公告）日：2022-06-30

  一种甾体偶联物，具体涉及一种化合物或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式，或其可药用的盐及其制备方法和应用。
• METHODS FOR THE ACYLATION OF MAYTANSINOL
  申请人：ImmunoGen, Inc.

  公开号：US20170137440A1

  公开（公告）日：2017-05-18

  Disclosed is a method of preparing an amino acid ester of maytansinol by reacting maytansinol with an N-carboxyanhydride of an amino acid (NCA) in the presence of a drying agent. Also disclosed is an improved method of preparing an amino acid ester of maytansinol in which a nucleophile is added to the reaction mixture after completion of the reaction between maytansinol and an N-carboxyanhydride of an amino acid.
• US9796731B2
  申请人：——

  公开号：US9796731B2

  公开（公告）日：2017-10-24
• A mild synthesis of N-functionalised bromomaleimides, thiomaleimides and bromopyridazinediones
  作者：Lourdes Castañeda、Zoë V.F. Wright、Cristina Marculescu、Trang M. Tran、Vijay Chudasama、Antoine Maruani、Elizabeth A. Hull、João P.M. Nunes、Richard J. Fitzmaurice、Mark E.B. Smith、Lyn H. Jones、Stephen Caddick、James R. Baker

  DOI：10.1016/j.tetlet.2013.04.088

  日期：2013.7

  Bromomaleimides are useful building blocks in synthesis and powerful reagents for the selective chemical modification of proteins. A mild new synthesis of these reagents is described, along with the convenient transferability of the approach to dithiomaleimides and bromopyridazinediones. (c) 2013 The Authors. Published by Elsevier Ltd. All rights reserved.