5-benzylhexahydro-1H-furo[3,4-c]pyrrol-1-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 呋喃吡咯
• 英文名称: 5-benzylhexahydro-1H-furo[3,4-c]pyrrol-1-one
• 英文别名: 5-benzyl-hexahydro-1H-furo[3,4-c]pyrrol-1-one；5-benzyl-3a,4,6,6a-tetrahydro-1H-furo[3,4-c]pyrrol-3-one
• 化学式: C₁₃H₁₅NO₂
• mdl: MFCD05662787
• 分子量: 217.268
• InChiKey: BZOLMBUOVVXGMF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.461
• 拓扑面积：
  29.5
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-benzylhexahydro-1H-furo[3,4-c]pyrrol-1-one 在 盐酸 、 tris-(dibenzylideneacetone)dipalladium(0) 、 palladium on activated charcoal 、 氢气 、 caesium carbonate 、 4,5-双二苯基膦-9,9-二甲基氧杂蒽 作用下， 以 1,4-二氧六环 、 甲醇 、 甲苯 为溶剂， 20.0~100.0 ℃ 、344.75 kPa 条件下， 反应 32.0h， 生成 5-(3,5-dichlorophenyl)hexahydro-1H-furo[3,4-c]pyrrol-1-one
  参考文献：
  名称：

  WO2020036940A5

  摘要：

  公开号：

  WO2020036940A5
• 作为产物：
  描述：

  2(5H)-呋喃酮 、 N-(甲氧甲基)-N-(三甲基硅甲基)苄胺 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 16.0h， 以41.3%的产率得到5-benzylhexahydro-1H-furo[3,4-c]pyrrol-1-one
  参考文献：
  名称：

  WO2020036940A5

  摘要：

  公开号：

  WO2020036940A5

文献信息

• Organic Compounds
  申请人：Ehrhardt Claus

  公开号：US20080194549A1

  公开（公告）日：2008-08-14

  The invention relates to the use of (3,4-di-, 3,3,4-tri, 3,4,4-tri- or 3,3,4,4-tetra-)substituted pyrrolidine compounds for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; compounds that are part of a subclass of these substituted pyrrolidine 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 activity of renin; new compounds that are part of a subclass of these substituted pyrrolidine compounds; pharmaceutical formulations comprising said substituted pyrrolidine compounds, and/or a method of treatment comprising administering said substituted pyrrolidine compounds, a method for the manufacture especially of said new substituted pyrrolidine compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesis.

  本发明涉及使用(3,4-二-, 3,3,4-三-, 3,4,4-三-或3,3,4,4-四-)取代吡咯烷化合物制备治疗依赖于肾素活性的疾病的药物制剂；使用该类化合物治疗依赖于肾素活性的疾病；该取代吡咯烷化合物亚类的化合物用于温血动物的诊断和治疗，特别是用于治疗依赖于肾素活性的疾病；该取代吡咯烷化合物亚类的新化合物；包括所述取代吡咯烷化合物的药物制剂和/或包括给予所述取代吡咯烷化合物的治疗方法，特别是制备该新取代吡咯烷化合物的方法，以及其合成的新中间体、起始材料和/或部分步骤。
• Fused substituted aminopyrrolidine derivative
  申请人：Takahashi Hisashi

  公开号：US20120108582A1

  公开（公告）日：2012-05-03

  A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure.

  提供了一种具有极好药物特性的喹诺酮合成抗菌剂，其不仅对革兰氏阴性菌具有强烈的抗菌活性，而且对对喹诺酮抗菌剂敏感度较低的革兰氏阳性球菌也具有强烈的抗菌活性，并表现出高安全性和优异的药代动力学特性。该化合物由式(I)或其盐或水合物表示，具体而言，是式(I)的喹诺酮衍生物，其中取代基R6和R7与它们所连接的碳原子一起形成一个环状结构，该环状结构可能包含一个氧原子作为环状成分原子，该环状结构形成一个5-4、5-5或5-6融合的双环吡咯烷基取代物，该取代物与含有吡啶苯并噁嗪结构的喹诺酮母骨架Q连接。
• Fused Substituted Aminopyrrolidine Derivative
  申请人：Daiichi Sankyo Company, Limited

  公开号：US20140142096A1

  公开（公告）日：2014-05-22

  A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure.

  提供了一种具有出色药物特性的喹诺酮合成抗菌剂，它不仅对革兰氏阴性菌具有强烈的抗菌活性，而且对对喹诺酮抗菌剂敏感性较低的革兰氏阳性球菌也具有强烈的抗菌活性，并且具有高安全性和优异的药代动力学。化合物由式(I)或其盐或其水合物表示，具体来说，是式(I)的喹诺酮衍生物，其中取代基R6和R7与它们连接的碳原子一起形成一个环状结构，该环状结构可以包含一个氧原子作为环构成原子，该环状结构形成一个5-4、5-5或5-6融合的双环吡咯烷基取代基，该取代基与含有吡啶并苯并噁嗪结构的喹诺酮母骨架Q连接。
• 3,4-SUBSTITUTED PYRROLIDINE DERIVATIVES FOR THE TREATMENT OF HYPERTENSION
  申请人：Novartis AG

  公开号：EP1863477A1

  公开（公告）日：2007-12-12
• FUSED SUBSTITUTED AMINOPYRROLIDINE DERIVATIVE
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP2097400B1

  公开（公告）日：2013-07-03