(2,5-Dioxopyrrolidin-1-yl) 4-benzylbenzoate | 852812-44-3

• 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: (2,5-Dioxopyrrolidin-1-yl) 4-benzylbenzoate
• CAS: 852812-44-3
• 化学式: C₁₈H₁₅NO₄
• 分子量: 309.321
• InChiKey: QWTSPAABDMBNGP-UHFFFAOYSA-N

物化性质

• 沸点：
  465.1±48.0 °C(Predicted)
• 密度：
  1.32±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  23
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  63.7
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (2,5-Dioxopyrrolidin-1-yl) 4-benzylbenzoate 在 N,N-二异丙基乙胺 作用下， 生成 (S)-3-(4-Benzyl-benzoylamino)-2-tert-butoxycarbonylamino-propionic acid methyl ester
  参考文献：
  名称：

  Synthesis and biological activities of aryl-ether-, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT-2

  摘要：

  Excitatory amino acid transporters (EAATs) play a pivotal role in maintaining glutamate homeostasis in the mammalian central nervous system, with the EAAT-2 subtype thought to be responsible for the bulk of the glutamate uptake in forebrain regions. A complete elucidation of the functional role of EAAT-2 has been hampered by the lack of potent and selective pharmacological tools. In this study, we describe the synthesis and biological activities of novel aryl-ether, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of EAAT-2. Compound (16) represents one of the most potent (IC50 = 85 +/- 5 nM) and selective inhibitors of EAAT-2 identified to date. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.08.003
• 作为产物：
  描述：

  N-羟基丁二酰亚胺 、 4-(苯基甲基)苯甲酸 在 N,N'-二异丙基碳二亚胺 作用下， 以 二氯甲烷 为溶剂， 生成 (2,5-Dioxopyrrolidin-1-yl) 4-benzylbenzoate
  参考文献：
  名称：

  Synthesis and biological activities of aryl-ether-, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT-2

  摘要：

  Excitatory amino acid transporters (EAATs) play a pivotal role in maintaining glutamate homeostasis in the mammalian central nervous system, with the EAAT-2 subtype thought to be responsible for the bulk of the glutamate uptake in forebrain regions. A complete elucidation of the functional role of EAAT-2 has been hampered by the lack of potent and selective pharmacological tools. In this study, we describe the synthesis and biological activities of novel aryl-ether, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of EAAT-2. Compound (16) represents one of the most potent (IC50 = 85 +/- 5 nM) and selective inhibitors of EAAT-2 identified to date. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.08.003

文献信息

• FORMATION OF 18F AND 19F FLUOROARENES BEARING REACTIVE FUNCTIONALITIES
  申请人：Carroll Michael Andrew

  公开号：US20090286992A1

  公开（公告）日：2009-11-19

  An iodonium compound of formula (I): where R AR1 is a C 5-6 aryl group, bearing at least one substituent selected from formyl, thionoacyl, acylamidocarboxy, thionoester, azo, C 2-20 alkenyl, C 2-20 alkynyl, and (CH 2 ) n R C , where R C is selected from ether, amino, azo and thioether; R AR2 is a C 5-10 aryl group, optionally substituted by one or more groups selected from C 1-12 alkyl, C 5-12 aryl, C 3-12 heterocyclyl, ether, thioether, nitro, cyano and halo, and may be linked to a solid support or fluorous tag; and X is a counteranion.

  化学式(I)的碘化物：其中RAR1是一个C5-6芳基，至少带有一种取代基，选自甲酰基、硫代酰基、酰胺羧基、硫酯、偶氮、C2-20烯基、C2-20炔基和(CH2)nRC，其中RC选自醚、氨基、偶氮和硫醚；RAR2是一个C5-10芳基，可选择地被一个或多个取代基取代，选自C1-12烷基、C5-12芳基、C3-12杂环烷基、醚、硫醚、硝基、氰基和卤素，并且可以连接到固体支撑物或氟标记；X是一个对阴离子。
• US8093405B2
  申请人：——

  公开号：US8093405B2

  公开（公告）日：2012-01-10
• [EN] RADIOIODINATED COMPOUNDS<br/>[FR] COMPOSÉS RADIOIODÉS
  申请人：NUTECH VENTURES

  公开号：WO2015147950A2

  公开（公告）日：2015-10-01

  This disclosure relates to reagents and methods useful in the synthesis of aryl iodines, for example, in the preparation of iodine labeled radiotracers. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.
• Synthesis and biological activities of aryl-ether-, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT-2
  作者：Alexander Greenfield、Cristina Grosanu、John Dunlop、Beal McIlvain、Tikva Carrick、Brian Jow、Qiang Lu、Dianne Kowal、John Williams、John Butera

  DOI：10.1016/j.bmcl.2005.08.003

  日期：2005.11

  Excitatory amino acid transporters (EAATs) play a pivotal role in maintaining glutamate homeostasis in the mammalian central nervous system, with the EAAT-2 subtype thought to be responsible for the bulk of the glutamate uptake in forebrain regions. A complete elucidation of the functional role of EAAT-2 has been hampered by the lack of potent and selective pharmacological tools. In this study, we describe the synthesis and biological activities of novel aryl-ether, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of EAAT-2. Compound (16) represents one of the most potent (IC50 = 85 +/- 5 nM) and selective inhibitors of EAAT-2 identified to date. (c) 2005 Elsevier Ltd. All rights reserved.