(3R,4R)-1,4-Dibenzyl-pyrrolidine-3-carboxylic acid | 218431-87-9

• 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: (3R,4R)-1,4-Dibenzyl-pyrrolidine-3-carboxylic acid
• 英文别名: (3R*,4R*)-1,4-dibenzyl-pyrrolidine-3-carboxylic acid；(3R,4R)-1,4-dibenzylpyrrolidine-3-carboxylic acid
• CAS: 218431-87-9
• 化学式: C₁₉H₂₁NO₂
• 分子量: 295.381
• InChiKey: VGJHMAVFQJLHKA-ROUUACIJSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  22
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  40.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (3R,4R)-1,4-Dibenzyl-pyrrolidine-3-carboxylic acid 在 N-甲基吗啉 作用下， 以 四氢呋喃 为溶剂， 反应 1.0h， 生成
  参考文献：
  名称：

  β-Analogs of PLG (l-prolyl-l-leucyl-glycinamide): Ex-chiral pool syntheses and dopamine D2 receptor modulating effects

  摘要：

  Starting from (S)- and (R)-aspartic acid enantiomerically pure P-proline derivatives were synthesized. These chiral building blocks were transformed into P-analogs of the dopamine receptor modulating peptide PLG. According to dopamine receptor binding studies, significant enhancement of [H-3]pramipexole binding was observed for the isomeres 1a,b and 2a-c. The derivative Ib revealed an activity comparable to PLG. (C) 1998 Elsevier Science Ltd. Air rights reserved.

  DOI：

  10.1016/s0960-894x(98)00507-1
• 作为产物：
  描述：

  在 盐酸 、 18-冠醚-6 作用下， 以 二甲基亚砜 为溶剂， 反应 188.0h， 生成 (3R,4R)-1,4-Dibenzyl-pyrrolidine-3-carboxylic acid
  参考文献：
  名称：

  β-Analogs of PLG (l-prolyl-l-leucyl-glycinamide): Ex-chiral pool syntheses and dopamine D2 receptor modulating effects

  摘要：

  Starting from (S)- and (R)-aspartic acid enantiomerically pure P-proline derivatives were synthesized. These chiral building blocks were transformed into P-analogs of the dopamine receptor modulating peptide PLG. According to dopamine receptor binding studies, significant enhancement of [H-3]pramipexole binding was observed for the isomeres 1a,b and 2a-c. The derivative Ib revealed an activity comparable to PLG. (C) 1998 Elsevier Science Ltd. Air rights reserved.

  DOI：

  10.1016/s0960-894x(98)00507-1

文献信息

• AMIDE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
  申请人：ESTEVE PHARMACEUTICALS, S.A.

  公开号：EP3858439A1

  公开（公告）日：2021-08-04

  The present invention relates to new compounds that show pharmacological activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels or dual activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels, and the µ-opiod receptor (MOR or mu-opioid). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.

  本发明涉及对电压门控钙通道（VGCC）的亚单位α2δ，特别是对电压门控钙通道的α2δ-1亚单位或对电压门控钙通道（VGCC）的亚单位α2δ以及µ-阿片受体（MOR或μ-阿片）显示药理活性的新化合物。该发明还涉及所述化合物的制备方法，以及包含它们的组合物，以及它们作为药物的用途。
• PYRROLIDINE DERIVATIVES USEFUL AS BACE INHIBITORS
  申请人：Rogel Olivier

  公开号：US20090247577A1

  公开（公告）日：2009-10-01

  Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (disorder) that depends on the activity of beta-secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on the activity of beta-secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound. The substituted pyrrolidine compounds are especially of the formula I, wherein the substituents are as defined in the specification.

  小说3-单取代、3,4-双取代和3,4,4-三取代吡咯烷化合物，这些化合物用于诊断和治疗温血动物，特别是用于治疗依赖于β-分泌酶活性和/或β-淀粉样蛋白生成及其后续寡聚体和纤维聚集的疾病（紊乱）；该类化合物的使用用于制备用于治疗依赖于β-分泌酶活性和/或β-淀粉样蛋白生成及其后续寡聚体和纤维聚集的疾病的药物配方；包括所述取代的吡咯烷化合物的药物配方和/或包括给予该取代的吡咯烷化合物的治疗方法。所述取代的吡咯烷化合物特别是公式I的，其中取代基如规范中所定义。
• Organic Compounds and Their Uses
  申请人：Brandl Trixi

  公开号：US20080045530A1

  公开（公告）日：2008-02-21

  The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.

  本申请描述了有机化合物，可用于治疗、预防和/或改善人类疾病。
• PYRROLIDINE DERIVATIVES FOR THE TREATMENT OF A DISEASE DEPENDING ON THE ACTIVITY OF RENIN
  申请人：Breitenstein Werner

  公开号：US20100087427A1

  公开（公告）日：2010-04-08

  Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.

  小说3-单一、3,4-二和3,4,4-三取代吡咯烷化合物，这些化合物用于诊断和治疗温血动物，特别是用于治疗依赖于肾素不适当活性的疾病（=失调）；该类化合物用于制备用于治疗依赖于肾素不适当活性的疾病的制药配方；该类化合物用于治疗依赖于肾素不适当活性的疾病；包括所述取代吡咯烷化合物的制药配方和/或包括给予所述取代吡咯烷化合物的治疗方法，以及描述了制备所述取代吡咯烷化合物的新型中间体和部分步骤。所述取代吡咯烷化合物特别是公式I的取代基如说明书所述。
• HCV INHIBITORS COMPRISING BETA AMINO ACIDS AND THEIR USES
  申请人：NOVARTIS AG

  公开号：EP2007787A2

  公开（公告）日：2008-12-31