diisopropyl azodicarboxylate | 2152653-55-7

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: diisopropyl azodicarboxylate
• 英文别名: DIAD；(Z)-diisopropyl diazene-1,2-dicarboxylate；propan-2-yl (NZ)-N-propan-2-yloxycarbonyliminocarbamate
• CAS: 2152653-55-7
• 化学式: C₈H₁₄N₂O₄
• 分子量: 202.21
• InChiKey: VVWRJUBEIPHGQF-KTKRTIGZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  77.3
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  diisopropyl azodicarboxylate 在 对甲苯磺酸 作用下， 以 苯 为溶剂， 反应 12.05h， 生成 (4R, 5S)-5-<1,2-bis(isopropoxycarbonyl)hydrazino>-4-methoxy-3-<(1S)-2-exo-methoxy-1-apocamphanecarbonyl>-2-oxazolidinone
  参考文献：
  名称：

  Chiral electrophilic “glycinal” equivalents. New synthons for optically active α-amino acids and 4-substituted 2-oxazolidinones

  摘要：

  The thermal reaction of 3-[(IS)-2-alkoxy-1-apocamphanecarbonyl]-2-oxazolones (21a-c) with dialkyl azodicarboxylates (9) results in exclusive formation of [4 + 2] type cycloadducts (22 and 23) with moderate levels of diastereofacial selection (up to 72% d.e.). The diastereomers thus obtained were readily purified and subsequent treatment with acidic methanol followed by removal of the auxiliary with LiBH4/MeOH (1:2) gave optically pure 4-methoxy-5-hydrazino-2-oxazolidinones (26 and 27), which serve as alpha-aminoaldehyde templates useful for the synthesis of a wide variety of optically active alpha-amino acids as well as 4-alkyl and 4-aryl-2-oxazolidinones. (C) 1997, Elsevier Science Ltd.

  DOI：

  10.1016/s0040-4020(96)01077-0
• 作为试剂：
  描述：

  2,3-二氟苯酚 、 (6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)chroman-2-yl)methanol 在 diisopropyl azodicarboxylate 、 三苯基膦 作用下， 以 四氢呋喃 为溶剂， 反应 1.17h， 以72.1%的产率得到2-(2-((2,3-difluorophenoxy)methyl)chroman-6-yl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane
  参考文献：
  名称：

  [EN] PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
  [FR] DÉRIVÉS D'ACIDE PYRIDIN-3-YLE ACÉTIQUE UTILISÉS COMME INHIBITEURS DE LA RÉPLICATION DU VIRUS DE L'IMMUNODÉFICIENCE HUMAINE

  摘要：

  公开了Formula I的化合物，包括药用可接受的盐，包含这些化合物的药物组合物，制备这些化合物的方法，以及它们在抑制HIV整合酶和治疗HIV或艾滋病感染者中的用途。

  公开号：

  WO2017195113A1

文献信息

• [EN] BIARYL COMPOUNDS USEFUL AS IMMUNOMODULATORS<br/>[FR] COMPOSÉS BIARYLES UTILES EN TANT QU'IMMUNOMODULATEURS
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2018044963A1

  公开（公告）日：2018-03-08

  The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.

  本公开涉及通常用作免疫调节剂的化合物。本文提供了包含这些化合物的组合物，以及它们的使用方法。该公开进一步涉及包含至少一种根据本公开的化合物的药物组合物，用于治疗各种疾病，包括癌症和传染病。
• [EN] MODULATORS OF THE GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO<br/>[FR] MODULATEURS DU RÉCEPTEUR GPR119 ET TRAITEMENT DE TROUBLES ASSOCIÉS
  申请人：ARENA PHARM INC

  公开号：WO2013055910A1

  公开（公告）日：2013-04-18

  The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, and N-oxides thereof,that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing secretion of an incretin; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.

  本发明涉及式(I)的化合物及其药学上可接受的盐、溶剂化合物、水合物和N-氧化物，这些化合物可作为单一药物代理或与一个或多个额外的药物代理结合使用，例如DPP-IV的抑制剂、双胍类药物、α-葡萄糖苷酶抑制剂、胰岛素类似物、磺脲类药物、SGLT2抑制剂、噻嗪二酮类药物或抗糖尿病肽类似物，用于治疗例如从以下选择的疾病中选择的疾病：GPR119受体相关疾病；通过增加促胰高血糖素分泌而改善的状况；通过增加血液促胰高血糖素水平而改善的状况；低骨量状况；神经系统疾病；与代谢相关的疾病；2型糖尿病；肥胖症；以及相关并发症。
• [EN] CYCLIC DI-NUCLEOTIDE COMPOUNDS AS STING AGONISTS<br/>[FR] COMPOSÉS DI-NUCLÉOTIDIQUES CYCLIQUES UTILISÉS EN TANT QU'AGONISTES DE STING
  申请人：MERCK SHARP & DOHME

  公开号：WO2020117625A1

  公开（公告）日：2020-06-11

  A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2a, R3, R3a, R4, R4a, R5, R6, R6a, R7, R7a, R8, R8a, and R9 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds. (I)

  提供一类多环化合物，其一般式为（I），其中Base1、Base2、Y、Ya、Xa、Xa1、Xb、Xb1、Xc、Xc1、Xd、Xd1、R1、R1a、R2a、R3、R3a、R4、R4a、R5、R6、R6a、R7、R7a、R8、R8a和R9在此处定义，可能有用作I型干扰素产生的诱导剂，特别是作为STING活性剂。还提供了合成和使用化合物的方法。（I）
• AMINOPYRIMIDINE COMPOUND
  申请人：Cardurion Pharmaceuticals, LLC

  公开号：US20200095240A1

  公开（公告）日：2020-03-26

  The present invention provides a compound having a CaMKII inhibitory action, which is expected to be useful as an agent for the prophylaxis or treatment of cardiac diseases (particularly catecholaminergic polymorphic ventricular tachycardia, postoperative atrial fibrillation, heart failure, fatal arrhythmia) and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

  本发明提供了一种具有CaMKII抑制作用的化合物，预计可用作心脏疾病（特别是儿茶酚胺多形性室性心动过速、术后心房颤动、心力衰竭、致命性心律失常等）的预防或治疗药物。本发明涉及一种由以下公式（I）表示的化合物：其中每个符号如规范中所定义，或其盐。
• [EN] SUBSTITUTED ISOQUIONLINE DERIVATIVES AS IMMUNOMUDULATORS<br/>[FR] DÉRIVÉS D'ISOQUINOLÉINE SUBSTITUÉS UTILISÉS EN TANT QU'IMMUNOMUTATEURS
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2018183171A1

  公开（公告）日：2018-10-04

  The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases. (I)

  本公开涉及通常用作免疫调节剂的化合物。提供的是包含这些化合物的组合物，以及它们的使用方法。本公开还涉及包含至少一种根据本公开的化合物的制药组合物，其用于治疗各种疾病，包括癌症和传染病。(I)