苄基(2,5-二氧代-3-吡咯烷基)氨基甲酸酯 | 84767-67-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 苄基(2,5-二氧代-3-吡咯烷基)氨基甲酸酯
• 英文名称: 3-[(benzyloxy)carbonylamino]pyrrolidine-2,5-dione
• 英文别名: benzyl (2,5-dioxopyrrolidin-3-yl)carbamate；(2,5-dioxo-pyrrolidin-3-yl)-carbamic acid benzyl ester；benzyl N-(2,5-dioxopyrrolidin-3-yl)carbamate
• CAS: 84767-67-9
• 化学式: C₁₂H₁₂N₂O₄
• 分子量: 248.238
• InChiKey: QRQMHYISDDHZBY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  84.5
• 氢给体数：
  2
• 氢受体数：
  4

安全信息

• 海关编码：
  2925190090

反应信息

• 作为反应物：
  描述：

  苄基(2,5-二氧代-3-吡咯烷基)氨基甲酸酯 在 sodium tetrahydroborate 、 potassium tert-butylate 作用下， 以 水 、 N,N-二甲基甲酰胺 、 异丙醇 、 甲苯 为溶剂， 反应 5.25h， 生成 3-[(benzyloxy)carbonylamino]-4-hydroxy-N-methylbutanamide
  参考文献：
  名称：

  Synthesis and evaluation of anti-apoptotic activity of L-carnitine cyclic analogues and amino acid derivatives

  摘要：

  Two series of derivatives were synthesised. In one series (R)-4-hydroxy-2-pyrrolidinone was used as a mimic of cyclic L-carnitine analogue and in the second series 3-amino-2-piperidinone was used as a cyclic ornithine analogue. N-Benzyloxycarbonyl derivatives of some amino acids were also prepared. The newly synthesised compounds were tested for their ability to inhibit Fas-activated apoptosis of human Jurkatt T-cell line. The results confirm the previously described anti-apoptotic activity of carnitine and indicate new carnitine and amino acid analogues (1, 3, 6, 7, 20) that inhibit Fas-induced apoptosis.

  DOI：

  10.1016/j.farmac.2004.01.004
• 作为产物：
  描述：

  Z-DL-天冬酰胺酸 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 5.0h， 以77%的产率得到苄基(2,5-二氧代-3-吡咯烷基)氨基甲酸酯
  参考文献：
  名称：

  Synthesis and evaluation of anti-apoptotic activity of L-carnitine cyclic analogues and amino acid derivatives

  摘要：

  Two series of derivatives were synthesised. In one series (R)-4-hydroxy-2-pyrrolidinone was used as a mimic of cyclic L-carnitine analogue and in the second series 3-amino-2-piperidinone was used as a cyclic ornithine analogue. N-Benzyloxycarbonyl derivatives of some amino acids were also prepared. The newly synthesised compounds were tested for their ability to inhibit Fas-activated apoptosis of human Jurkatt T-cell line. The results confirm the previously described anti-apoptotic activity of carnitine and indicate new carnitine and amino acid analogues (1, 3, 6, 7, 20) that inhibit Fas-induced apoptosis.

  DOI：

  10.1016/j.farmac.2004.01.004

文献信息

• [EN] GLUCOSE RESPONSIVE INSULIN COMPRISING A TRI-VALENT SUGAR CLUSTER FOR TREATMENT OF DIABETES<br/>[FR] INSULINE SENSIBLE AU GLUCOSE COMPRENANT UN GROUPE DE SUCRE TRIVALENT POUR LE TRAITEMENT DU DIABÈTE
  申请人：MERCK SHARP & DOHME

  公开号：WO2018175272A1

  公开（公告）日：2018-09-27

  An insulin conjugate comprising or consisting of a tri-valent sugar cluster is described. In particular aspects, the insulin conjugate displays a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.

  描述了一种含有三价糖团的胰岛素共轭物。在特定方面，该胰岛素共轭物显示出对系统中的糖类浓度（如葡萄糖或α-甲基甘露糖）具有响应性的药代动力学（PK）和/或药效动力学（PD）特性，即使在向需要该胰岛素共轭物的受试者施用时，不需要外源多价糖类结合分子（如Con A）的存在。
• [EN] NEW HETEROCYCLIC AMIDE COMPOUNDS USEFUL FOR THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISORDERS: PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM<br/>[FR] NOUVEAUX COMPOSES AMIDES HETEROCYCLIQUES UTILISES POUR LE TRAITEMENT D'AFFECTIONS INFLAMMATOIRES ET ALLERGIQUES; PROCEDE PERMETTANT DE LES FABRIQUER ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT
  申请人：GLENMARK PHARMACEUTICALS LTD

  公开号：WO2004022536A1

  公开（公告）日：2004-03-18

  The present invention relates to novel heterocyclic compounds that inhibit phosphodiesterase type 4 (PDE 4). The compounds are useful for treating inflammatory conditions, diseases of the central nervous systems and insulin resistant diabetes.

  本发明涉及一种新型杂环化合物，可抑制磷酸二酯酶4型（PDE 4）。这些化合物可用于治疗炎症性疾病、中枢神经系统疾病和胰岛素抵抗性糖尿病。
• [EN] INHIBITORS OF APOL1 AND USE OF THE SAME<br/>[FR] INHIBITEURS D'APOL1 ET LEUR UTILISATION
  申请人：VERTEX PHARMA

  公开号：WO2021252849A1

  公开（公告）日：2021-12-16

  The disclosure provides compounds of Formula (I), deuterated derivatives of those compounds, and pharmaceutically acceptable salts of those compounds and derivatives, compositions comprising the same, and methods of using the same, including use in treating APOL1 mediated kidney disease.

  该披露提供了式（I）的化合物，这些化合物的氘代衍生物，以及这些化合物和衍生物的药用盐，包含这些化合物的组合物，以及使用这些化合物的方法，包括用于治疗APOL1介导的肾病。
• [EN] PREPARATION OF N-PROTECTED-3-PYRROLIDINE-LACTAM SUBSTITUTED PHOSPHONIUM SALTS<br/>[FR] PREPARATION DE SELS DE PHOSPHONIUM SUBSTITUES PAR 3-PYRROLIDINE-LACTAME N-PROTEGE
  申请人：BASILEA PHARMACEUTICA AG

  公开号：WO2002014332A1

  公开（公告）日：2002-02-21

  New process for the preparation of bipyrrolidinyl compounds of formula I wherein * signifies an asymmetric centre with an (R) or (S) configuration and X represents chlorine, bromine or iodine. The compounds of formula I are important building blocks for the production of useful products in the chemical and in the pharmaceutical industry. In particular they are useful for the production of antibacterial substances for example like vinylpyrrolidinone-cephalosporin derivatives.

  新的制备双吡咯烷基化合物I的方法，其中*表示具有(R)或(S)构型的不对称中心，X代表氯、溴或碘。公式I的化合物是化学和制药行业中生产有用产品的重要构建块。特别是它们对于生产抗菌物质非常有用，例如像乙烯基吡咯烷酮头孢菌素衍生物。
• Preparation of n-protected-3-pyrrolidine-lactam substituted phosphonium salts
  申请人：——

  公开号：US20030195364A1

  公开（公告）日：2003-10-16

  New process for the preparation of bipyrrolidinyl compounds of formula I wherein * signifies an asymmetric centre with an (R) or (S) configuration and X represents chlorine, bromine or iodine. The compounds of formula I are important building blocks for the production of useful products in the chemical and in the pharmaceutical industry. In particular they are useful for the production of antibacterial substances for example like vinylpyrrolidinone-cephalosporin derivatives. 1

  新的制备含有式I的双吡咯烷化合物的过程，其中*表示具有（R）或（S）构型的不对称中心，X代表氯，溴或碘。式I的化合物是化学和制药工业中生产有用产品的重要构建块。特别是它们对于生产抗菌物质非常有用，例如像乙烯吡咯烷酮头孢菌素衍生物。1