isovaleric acid N-oxysuccinimide ester | 282540-05-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: isovaleric acid N-oxysuccinimide ester
• 英文别名: succinimidyl isovalerate；1-[(3-Methylbutanoyl)oxy]pyrrolidine-2,5-dione；(2,5-dioxopyrrolidin-1-yl) 3-methylbutanoate
• CAS: 282540-05-0
• 化学式: C₉H₁₃NO₄
• mdl: MFCD22193830
• 分子量: 199.207
• InChiKey: YJRXBNGDPXLRLK-UHFFFAOYSA-N

物化性质

• 沸点：
  279.3±23.0 °C(Predicted)
• 密度：
  1.21±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.666
• 拓扑面积：
  63.7
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  isovaleric acid N-oxysuccinimide ester 在 羟胺 作用下， 以 水 、 乙腈 为溶剂， 反应 12.0h， 以436 mg的产率得到N-hydroxy-3-methylbutanamide
  参考文献：
  名称：

  由醛和羟胺一锅法合成异羟肟酸

  摘要：

  AbstractA one‐pot oxidative transformation of aldehydes into hydroxamic acids by the use of an aqueous solution of hydroxylamine is reported. The methodology gives high yields and makes use of cheap, abundant and easily available reagents.magnified image

  DOI：

  10.1002/adsc.201400188
• 作为产物：
  描述：

  异戊酸 、 N-羟基丁二酰亚胺 在 N,N'-二环己基碳二亚胺 作用下， 以 二氯甲烷 为溶剂， 反应 168.0h， 以90%的产率得到isovaleric acid N-oxysuccinimide ester
  参考文献：
  名称：

  Synthesis of N4-(2-acetamido-2-deoxy-β-d-glucopyranosyl)-l-asparagine analogues. n-Butyramide, 3-chloropropionamide, 3-aminopropionamide, and isovaleramide analogues

  摘要：

  The syntheses of four analogues of N-4-(2-acetamido-2-deoxy-beta -D-glucopyranosyl)-L-asparagine are described. Activated carboxylic acids were reacted with 2-acetamido-2-deoxy-beta -D-glucopyranosylamine, n-Butyric anhydride gave N-(2-acetamido-2-deoxy-beta -D-glucopyranosyl)-n-butyramide. 3-Chloropropionic anhydride was synthesized from 3-chloropropionic acid and gave N-(2-acetamido-2-deoxy-beta -D-glucopyranosyl)-3-chloropropionamide. Equilibration of the latter with ammonium bicarbonate gave N-1-(2-acetamido-2-deoxy-beta -D-glucopyranosyl)-3-aminopropionamide. Succinimidyl isovalerate was synthesized and gave N-(2-acetamido-2-deoxy-beta -D-glucopyranosyl)isovaleramide. (C) 2001 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0008-6215(01)00057-x

文献信息

• [EN] PI-3 KINASE INHIBITOR PRODRUGS<br/>[FR] PROMEDICAMENTS D'INHIBITEURS DE PI-3 KINASE
  申请人：SEMAFORE PHARMACEUTICALS INC

  公开号：WO2004089925A1

  公开（公告）日：2004-10-21

  The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.

  这项发明提供了PI-3激酶抑制剂的新型前药。这些新型化合物是LY294002及其类似物，包括可逆性季铵化胺。
• [EN] STABILITY-MODULATING LINKERS FOR USE WITH ANTIBODY DRUG CONJUGATES<br/>[FR] LIEURS MODULANT LA STABILITÉ DESTINÉS À ÊTRE UTILISÉS AVEC DES CONJUGUÉS ANTICORPS-MÉDICAMENT
  申请人：PFIZER

  公开号：WO2016030791A1

  公开（公告）日：2016-03-03

  The present invention provides stability-modulated antibody-drug conjugates, stability-modulating linker components used to make these stability-modulated antibody-drug conjugates, therapeutic methods using stability-modulated antibody-drug conjugates, and methods of making stability modulating linkers and stability-modulated antibody-drug conjugates.

  本发明提供了稳定性调节的抗体药物偶联物，用于制造这些稳定性调节的抗体药物偶联物的稳定性调节连接器组分，使用稳定性调节的抗体药物偶联物的治疗方法，以及制造稳定性调节连接器和稳定性调节的抗体药物偶联物的方法。
• PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF
  申请人：Medimmune Limited

  公开号：US20180134717A1

  公开（公告）日：2018-05-17

  Conjugates and compounds for making conjugates which are PBD molecules linked via the N10 position are disclosed, along with the use of the conjugates for treating proliferative diseases, including cancer.

  揭示了用于制备通过N10位置连接的PBD分子的共轭物和化合物，以及利用这些共轭物治疗增殖性疾病，包括癌症。
• HYBRID BLOCK COPOLYMER MICELLES WITH MIXED STEREOCHEMISTRY FOR ENCAPSULATION OF HYDROPHOBIC AGENTS
  申请人：SILL Kevin N.

  公开号：US20080274173A1

  公开（公告）日：2008-11-06

  The present invention relates to the field of polymer chemistry and more particularly to multiblock copolymers and micelles comprising the same.

  本发明涉及聚合物化学领域，更具体地说是涉及多嵌段共聚物以及包含该共聚物的胶束。
• FGF RECEPTOR-ACTIVATING N-ACYL OCTASACCHARIDES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
  申请人：DRIGUEZ Pierre Alexandre

  公开号：US20120214754A1

  公开（公告）日：2012-08-23

  The invention relates to FGF receptor-activating N-acyl octasaccharides having Formula (I), wherein: R 1 is an O-alkyl group optionally replaced by one or more aryl or cycloalkyl groups, R 2 is an OSO 3 − or hydroxyl group, R 3 is an alkyl, cycloalkyl, or alkyl-cycloalkyl group, R 4 is a disaccharide having Formula (II), R 6 is a disaccharide having Formula (III), and R 8 is a disaccharide having Formula (IV), where R 5 , R 7 , and R 9 are OSO 3 − or hydroxyl groups. The invention further relates to the preparation of said octasaccharides and to the therapeutic use thereof.

  该发明涉及具有化学式（I）的FGF受体激活N-酰基八糖，其中：R1是一个可选地由一个或多个芳基或环烷基取代的O-烷基基团，R2是一个OSO3−或羟基，R3是一个烷基、环烷基或烷基-环烷基基团，R4是具有化学式（II）的二糖，R6是具有化学式（III）的二糖，R8是具有化学式（IV）的二糖，其中R5、R7和R9是OSO3−或羟基基团。该发明还涉及所述八糖的制备以及其治疗用途。