4-phenyldihydro-3(2H)-furanone | 946125-02-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-phenyldihydro-3(2H)-furanone
• 英文别名: 4-phenyloxolan-3-one
• CAS: 946125-02-6
• 化学式: C₁₀H₁₀O₂
• 分子量: 162.188
• InChiKey: FIIIECQDPFHWKL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  26.3
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-phenyldihydro-3(2H)-furanone 、 苄胺 在 三乙酰氧基硼氢化钠 、 溶剂黄146 、 水 作用下， 以 二氯甲烷 为溶剂， 反应 18.67h， 生成 cis-4-phenyl-N-(phenylmethyl)tetrahydro-3-furanamine
  参考文献：
  名称：

  WO2007/90840

  摘要：

  公开号：
• 作为产物：
  描述：

  (3S,4R)-4-phenyltetrahydrofuran-3-ol 在 2,2,6,6-四甲基哌啶氧化物 、 三氯异氰尿酸 作用下， 以 二氯甲烷 为溶剂， 反应 3.0h， 生成 4-phenyldihydro-3(2H)-furanone
  参考文献：
  名称：

  WO2007/90840

  摘要：

  公开号：

文献信息

• [EN] 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS<br/>[FR] DÉRIVÉS DE 1,2,4-TRIAZOLO[4,3-A]PYRIDINE ET LEUR UTILISATION EN TANT QUE MODULATEURS ALLOSTÉRIQUES POSITIFS DES RÉCEPTEURS MGLUR2
  申请人：JANSSEN PHARMACEUTICALS INC

  公开号：WO2012062750A1

  公开（公告）日：2012-05-18

  The present invention relates to novel triazolo [4,3-a]pyridine derivatives of Formula (I), wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 ("mGluR2"), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.

  本发明涉及式(I)的新三唑[4,3-a]吡啶衍生物，其中所有基团均如权利要求中所定义。根据发明的化合物是代谢型谷氨酸受体2型("mGluR2")的正变构调节剂，用于治疗或预防与谷氨酸功能障碍相关的神经和精神障碍以及涉及mGluR2亚型的代谢型受体的疾病。本发明还涉及包含这些化合物的药物组合物，制备这些化合物和组合物的方法，以及使用这些化合物预防或治疗涉及mGluR2的神经和精神障碍和疾病。
• [EN] 2,6,7,8 SUBSTITUTED PURINES AS HDM2 INHIBITORS<br/>[FR] PURINES 2,6,7,8-SUBSTITUÉES UTILISÉES EN TANT QU'INHIBITEURS DE HDM2
  申请人：MERCK SHARP & DOHME

  公开号：WO2014120748A1

  公开（公告）日：2014-08-07

  The present invention provides 2,6,7,8 Substituted Purines as described herein or a pharmaceutically acceptable salt thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.

  本发明提供如本文所述的2,6,7,8取代嘌呤或其药学上可接受的盐。代表性化合物可用作HDM2蛋白的抑制剂。还公开了包括上述化合物的药物组合物以及使用它们治疗癌症的潜在方法。
• 4-PHENYL-3-(2-PROPYLSULFONYLAMINO) TETRAHYDROFURAN DERIVATIVES WHICH POTENTIATE GLUTAMATE RECEPTORS AND ARE USEFUL IN THE TREATMENT OF SCHIZOPHRENIA
  申请人：Thewlis Kevin Michael

  公开号：US20090221643A1

  公开（公告）日：2009-09-03

  Compounds of formula (I), salts and solvates thereof are provided: wherein Ar is selected from phenyl, pyridyl and thienyl optionally substituted with one or more groups Y; and each Y group is independently selected from the group consisting of: halo, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, cyano, C(O)C 1-4 alkyl, NHSO 2 C 1-4 alkyl, NMeSO 2 C 1-4 alkyl, NHCOC 1-4 alkyl, NMeCOC 1-4 alkyl, SOC 1-4 alkyl, SO 2 C 1-4 alkyl and CO 2 C 1-4 alkyl, or two Y groups together form a cyclic group —O(CH 2 )O—. Processes for preparation, and uses thereof in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.

  提供式(I)的化合物、盐和溶剂化物，其中Ar从苯基、吡啶基和噻吩基中选择，可选地用一个或多个Y基团取代；每个Y基团独立地从以下基团中选择：卤、C1-4烷基、卤代C1-4烷基、C1-4烷氧基、氰基、C（O）C1-4烷基、NHSO2C1-4烷基、NMeSO2C1-4烷基、NHCOC1-4烷基、NMeCOC1-4烷基、SOC1-4烷基、SO2C1-4烷基和CO2C1-4烷基，或两个Y基团共同形成一个环状基团- O（CH2）O-。还公开了制备过程以及在治疗由谷氨酸受体功能降低或不平衡介导的疾病或病症，例如精神分裂症或认知障碍中的用途。
• 2,6,7,8 SUBSTITUTED PURINES AS HDM2 INHIBITORS
  申请人：MERCK SHARP & DOHME CORP.

  公开号：US20150353553A1

  公开（公告）日：2015-12-10

  The present invention provides 2,6,7,8 Substituted Purines as described herein or a pharmaceutically acceptable salt thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.

  本发明提供了如本文所述的2,6,7,8取代嘌呤或其药学上可接受的盐。这些代表性化合物可用作HDM2蛋白的抑制剂。本发明还公开了包含上述化合物的药物组合物以及使用它们治疗癌症的潜在方法。
• N-Substituted pyrrolidines and tetrahydrofurans as novel AMPAR positive modulators
  作者：Kevin M. Thewlis、Laura Aldegheri、Mark H. Harries、Claudette Mookherjee、Beatrice Oliosi、Simon E. Ward

  DOI：10.1016/j.bmcl.2010.09.062

  日期：2010.12

  A series of novel AMPA receptor positive modulators displaying CNS penetration have been discovered with sub-micromolar activity and good selectivity over the cardiac channel receptor, hERG. We describe here the synthesis of these compounds which are biaryl pyrrolidine and tetrahydrofuran sulfonamides and disclose their activities against the human GluA2 flip isoform homotetrameric receptor. (C) 2010 Published by Elsevier Ltd.