4-dihydroxyborylstilbene | 250603-10-2

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: 4-dihydroxyborylstilbene
• 英文别名: Stilbene-4-boronic acid；4(E-2-phenylethenyl)phenylboronic acid；4-styrylphenylboronic acid；(E)-(4-Styrylphenyl)boronic acid；[4-[(E)-2-phenylethenyl]phenyl]boronic acid
• CAS: 250603-10-2
• 化学式: C₁₄H₁₃BO₂
• 分子量: 224.067
• InChiKey: RAHFHNVYCKLZGU-VOTSOKGWSA-N

物化性质

• 沸点：
  416.1±48.0 °C(Predicted)
• 密度：
  1.15±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.54
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  40.5
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  10,10’-二溴-9,9’-联二蒽 、 4-dihydroxyborylstilbene 在 Pd catalyst potassium carbonate 作用下， 以 四氢呋喃 、 甲苯 、 正丁醇 为溶剂， 反应 80.0h， 以82%的产率得到10,10'-distylbenylbiantryl
  参考文献：
  名称：

  Synthesis and optical properties of novel blue fluorescent conjugated polymers

  摘要：

  本文介绍了一种合成具有确定共轭长度的共轭聚合物的新方法，该聚合物能够产生蓝光或绿光荧光。所报道的新方法是利用1,3-亚苯基（类型1）和10,10′-联二蒽（类型2）作为共轭片段（如芪和噻吩）的桥接单元，这些片段的光学性质可以通过简单的变化进一步调整。

  DOI：

  10.1039/a808590k
• 作为产物：
  描述：

  (E)-4,4,5,5-tetramethyl-2-(4-styrylphenyl)-1,3,2-dioxaborolane 在 盐酸 、 polystyrene boronic acid 作用下， 以 乙腈 为溶剂， 反应 18.0h， 以94%的产率得到4-dihydroxyborylstilbene
  参考文献：
  名称：

  Deprotection of pinacolyl boronate esters by transesterification with polystyrene–boronic acid

  摘要：

  Mild deprotection of pinacolyl boronate esters to the corresponding boronic acids was achieved in the presence of excess polystyrene-boronic acid via a transesterification process. The procedure allows for the cleavage of pinacolyl boronate esters in the presence of sensitive functional groups. Crown Copyright (C) 2004 Published by Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2004.07.014

文献信息

• Differentially Protected Benzenediboronic Acids:  Divalent Cross-Coupling Modules for the Efficient Synthesis of Boron-Substituted Oligoarenes
  作者：Hiroyoshi Noguchi、Takayuki Shioda、Chih-Ming Chou、Michinori Suginome

  DOI：10.1021/ol702420x

  日期：2008.2.1

  boron-masking strategy, new divalent cross-coupling modules have been designed for the efficient synthesis of boron-substituted oligoarenes. The modules, i.e., monoprotected o-, m-, and p-benzenediboronic acid derivatives, undergo highly selective Suzuki-Miyaura coupling with sp2 iodides, bromides, chlorides, and triflates, affording coupling products in which the protected boronyl groups are left intact

  基于硼屏蔽策略，已设计出新的二价交叉偶联模块以有效合成硼取代的低聚芳烃。该模块，即单保护的邻，间和对苯二硼酸衍生物，经过高度选择性的Suzuki-Miyaura与sp2碘化物，溴化物，氯化物和三氟甲磺酸酯偶联，得到偶联产物，其中受保护的硼烷基保持完整。
• Lipopeptide Compounds and Their Use
  申请人：Boyce Rustum S.

  公开号：US20110224129A1

  公开（公告）日：2011-09-15

  The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain lipopeptide compounds comprising a cyclic peptide bearing a lipid side chain (for convenience, collectively referred to herein as “LP compounds”), which, inter alia, are antimicrobial, particularly antibacterial. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to provide an antimicrobial function, particularly an antibacterial function, and in the treatment of diseases and conditions that are mediated by microbes, particularly bacteria, that are ameliorated by the antimicrobial function, particularly an antibacterial function, including bacterial diseases, optionally in combination with another agent, for example, another antibacterial agent.

  本发明一般涉及治疗化合物领域，更具体地涉及包括带有脂肪侧链的环肽的某些脂肽化合物（为方便起见，在本文中统称为“LP化合物”），其中，这些化合物具有抗微生物作用，特别是抗菌作用。本发明还涉及包括这些化合物的药物组合物，以及使用这些化合物和组合物，在体外和体内提供抗微生物功能，特别是抗菌功能，以及在治疗由微生物介导的疾病和病症方面的用途，特别是由抗菌功能缓解的细菌疾病，可选地与另一药剂（例如另一抗菌剂）结合使用。
• Oxyiminoalkanoic acid derivatives
  申请人：——

  公开号：US20030186985A1

  公开（公告）日：2003-10-02

  To provide a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the prevention or treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance and impaired glucose tolerance. A compound represented by the formula: 1 wherein R 1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a bond, —CO—, —CH(OH)— or a group represented by —NR 6 — wherein R 6 is a hydrogen atom or an optionally substituted alkyl group; n is an integer of 1 to 3; Y is an oxygen atom, a sulfur atom, —SO—, —SO 2 — or a group represented by —NR 7 — wherein R 7 is a hydrogen atom or an optionally alkyl group; ring A is a benzene ring optionally having additional one to three substituents; p is an integer of 1 to 8; R 2 is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; q is an integer of 0 to 6; m is 0 or 1; R 3 is a hydroxy group, OR 8 (R 8 is an optionally substituted hydrocarbon group.) or NR 9 R 10 (R 9 and R 10 are the same or different groups which are selected from a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted acyl group or R 9 and R 10 combine together to form a ring); R 4 and R 5 are the same or different groups which are selected from a hydrogen atom or an optionally substituted hydrocarbon group wherein R 4 may form a ring with R 2 ; provided that when R 1 is a ethoxymethyl, a C 1-3 alkyl, phenyl or p-methoxyphenyl and q=m=0, R 3 is NR 9 R 10 ; and provided that O-[2-chloro-4-(2-quinolylmethoxy)phenylmethyl]oxime and a methylpyruvate of [2-chloro-4-(2-quinolylmethoxy)phenylmethyl]-2-iminoxypropionic acid are excluded; or a salt thereof.

  提供一种新型的氧亚胺基脂肪酸衍生物，具有出色的降血糖和降血脂作用，可用于预防或治疗糖尿病、高脂血症、胰岛素不敏感、胰岛素抵抗和糖耐量受损。该化合物由以下公式表示：1其中，R1是可选取代的碳氢基团或可选取代的杂环基团；X是键，-CO-，-CH(OH)-或由-NR6-表示的基团（其中R6是氢原子或可选取代的烷基）；n是1至3的整数；Y是氧原子、硫原子、-SO-，-SO2-或由-NR7-表示的基团（其中R7是氢原子或可选的烷基）；环A是苯环，可选地具有额外的1至3个取代基；p是1至8的整数；R2是氢原子、可选取代的碳氢基团或可选取代的杂环基团；q是0至6的整数；m是0或1；R3是羟基、OR8（其中R8是可选取代的碳氢基团）或NR9R10（其中R9和R10是从氢原子、可选取代的碳氢基团、可选取代的杂环基团或可选取代的酰基中选择的相同或不同基团，或R9和R10结合形成环）；R4和R5是从氢原子或可选取代的碳氢基团中选择的相同或不同基团，其中R4可以与R2形成环；但当R1为乙氧甲基、C1-3烷基、苯基或对甲氧基苯基且q=m=0时，R3为NR9R10；并且不包括O-[2-氯-4-(2-喹啉基甲氧基)苯基甲基]肟和[2-氯-4-(2-喹啉基甲氧基)苯基甲基]-2-亚氨基丙酸甲酯，或其盐。
• Oxyiminoalkanoic acid derivatives with hypoglycemic and hypolipidemic activity
  申请人：Takeda Chemical Industries, Ltd.

  公开号：US06251926B1

  公开（公告）日：2001-06-26

  This invention provides a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance and impaired glucose tolerance.

  该发明提供了一种新型的氧亚胺基烷酸衍生物，具有优秀的降血糖和降血脂作用，可用于治疗糖尿病、高脂血症、胰岛素不敏感、胰岛素抵抗和糖耐量受损。
• Pyranone, Thiopyranone, and Pyridone Inhibitors of Phosphatidylinositol 3-Kinase Related Kinases. Structure−Activity Relationships for DNA-Dependent Protein Kinase Inhibition, and Identification of the First Potent and Selective Inhibitor of the Ataxia Telangiectasia Mutated Kinase
  作者：Jonathan J. Hollick、Laurent J. M. Rigoreau、Celine Cano-Soumillac、Xiaoling Cockcroft、Nicola J. Curtin、Mark Frigerio、Bernard T. Golding、Sophie Guiard、Ian R. Hardcastle、Ian Hickson、Marc G. Hummersone、Keith A. Menear、Niall M. B. Martin、Ian Matthews、David R. Newell、Rachel Ord、Caroline J. Richardson、Graeme C. M. Smith、Roger J. Griffin

  DOI：10.1021/jm061121y

  日期：2007.4.1

  Structure-activity relationships have been investigated for inhibition of DNA-dependent protein kinase (DNA-PK) and ATM kinase by a series of pyran-2-ones, pyran-4-ones, thiopyran-4-ones, and pyridin-4-ones. A wide range of IC50 values were observed for pyranones and thiopyranones substituted at the 6-position, with the 3- and 5-positions proving intolerant to substitution. Related pyran-2-ones, pyran-4-ones, and thiopyran-4-ones showed similar IC50 values against DNA-PK, whereas the pyridin-4-one system proved, in general, ineffective at inhibiting DNA-PK. Extended libraries exploring the 6-position of 2-morpholino-pyran-4-ones and 2-morpholino-thiopyrano-4-ones identified the first highly potent and selective ATM inhibitor 2-morpholin-4-yl-6-thianthren-1-yl-pyran-4-one (151C; ATM; IC50 = 13 nM) and revealed constrained SARs for ATM inhibition compared with DNA-PK. One of the most potent DNA-PK inhibitors identified, 2-(4-methoxyphenyl)-6-(morpholin-4-yl)pyran-4-one (16; DNA-PK; IC50 = 220 nM) effectively sensitized HeLa cells to the topoisomerase II inhibitor etoposide in vitro.