4'-Hydroxy-3-methyl-benzophenon | 71372-37-7

• 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'-Hydroxy-3-methyl-benzophenon
• 英文别名: 4-Hydroxy-3'-methylbenzophenone；(4-hydroxyphenyl)-(3-methylphenyl)methanone
• CAS: 71372-37-7
• 化学式: C₁₄H₁₂O₂
• 分子量: 212.248
• InChiKey: SONRRMLXSPQLND-UHFFFAOYSA-N

物化性质

• 熔点：
  166°C
• 沸点：
  394.8±35.0 °C(Predicted)
• 密度：
  1.164±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  37.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4'-Hydroxy-3-methyl-benzophenon 在 potassium carbonate 、 potassium iodide 作用下， 以 丁酮 为溶剂， 反应 96.0h， 生成 Ethyl 4-[3-[4-(3-methylbenzoyl)phenoxy]propyl]piperazine-1-carboxylate
  参考文献：
  名称：

  Structure–activity relationships of non-imidazole H3 receptor ligands. Part 1

  摘要：

  SAR studies for novel non-imidazole containing H-3 receptor antagonists with high potency and selectivity for rat H-3 receptors are described. A high throughput screening lead, A-923, was further elaborated in a systematic manner to clarify a pharmacophore for this class of aryloxyalkyl piperazine based compounds. (C) 2002 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(02)00309-8
• 作为产物：
  描述：

  苯甲醚 在 ytterbium(III) triflate 、 sodium thiomethoxide 作用下， 以 硝基甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 13.0h， 生成 4'-Hydroxy-3-methyl-benzophenon
  参考文献：
  名称：

  Synthesis and structure–activity relationship for new series of 4-Phenoxyquinoline derivatives as specific inhibitors of platelet-derived growth factor receptor tyrosine kinase

  摘要：

  We discovered a new series of 4-phenoxyquinoline derivatives as potent and selective inhibitors of the platelet-derived growth factor receptor (PDGFr) tyrosine kinase. We researched the highly potent and selective inhibitors on the basis of both PDGFr and epidermal growth factor receptor (EGFr) inhibitory activity. First, we found a compound, Ki6783 (1), which inhibited PDGFr autophosphorylation at 0.13 muM, but it did not inhibit EGFr autophosphorylation at 100 muM. After extensive explorations, we found the two desired compounds, Ki6896 (2) and Ki6945 (3), which are substituted by benzoyl and benzamide at the 4-position of the phenoxy group on 4-phenoxyquinoline, respectively. These inhibitory activities were 0.31 and 0.050 muM, respectively, but neither of them inhibited EGFr autophosphorylation at 100 M. We further investigated the profile of both compounds toward various tyrosine and serine/threonine kinases. The three compounds specifically inhibited PDGFr rather than the other kinases. (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2003.08.020

文献信息

• [EN] PHOTOACTIVATABLE FOULING-RESISTANT COPOLYMERS<br/>[FR] COPOLYMÈRES RÉSISTANT À L'ENCRASSEMENT PHOTOACTIVABLES
  申请人：ARROW INT INC

  公开号：WO2017030950A1

  公开（公告）日：2017-02-23

  A photoactivatable fouling-resistant copolymer composed of a photoactivatable monomer and a hydrophilic monomer is disclosed. The photoactivatable monomer includes an aryl ketone derivative having one or more polar groups or alkyl groups.

  一种由光活化单体和亲水单体组成的光活化防污共聚物被披露。光活化单体包括具有一个或多个极性基团或烷基基团的芳基酮衍生物。
• Advanced palladium free approach to the synthesis of substituted alkene oxindoles <i>via</i> aluminum-promoted Knoevenagel reaction
  作者：Daria S. Novikova、Tatyana A. Grigoreva、Andrey A. Zolotarev、Alexander V. Garabadzhiu、Vyacheslav G. Tribulovich

  DOI：10.1039/c8ra07576j

  日期：——

  A synthetic route for the synthesis of C24, as well as for the design of focused libraries of direct AMPK activators was developed based on a convergent strategy. The proposed scheme corresponds to the current trends in C–H bond functionalization. The use of aluminum isopropoxide for the Knoevenagel condensation of oxindole with benzophenones is a noticeable point of this work.

  基于收敛策略开发了用于合成 C24 以及设计直接 AMPK 激活剂的重点文库的合成路线。所提出的方案对应于 C-H 键功能化的当前趋势。异丙醇铝用于羟吲哚与二苯甲酮的 Knoevenagel 缩合是这项工作的一个显着点。
• Compound having tgfß inhibitory activity and medicinal composition containing the same
  申请人：Shimizu Kiyoshi

  公开号：US20060111375A1

  公开（公告）日：2006-05-25

  The present invention provides compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein X represents CH or N; Z represents —O—, —NH— or —C(═O)—; R and R′ represent a hydrogen atom, hydroxyl, a halogen atom, optionally substituted alkyl, optionally substituted alkenyl optionally substituted alkoxy, amino, aminocarbonyl, or an optionally substituted heterocyclic group; and A represents an optionally substituted specific carbocyclic or heterocyclic group. The compounds according to the present invention have excellent TGFβ inhibitory activity.

  本发明提供了以下公式（I）所表示的化合物及其药学上可接受的盐和溶剂： 其中，X代表CH或N；Z代表-O-，-NH-或-C（=O）-；R和R'代表氢原子，羟基，卤原子，可选择取代的烷基，可选择取代的烯基，可选择取代的烷氧基，氨基，氨基甲酰基或可选择取代的杂环基；A代表可选择取代的特定环烷基或杂环基。本发明的化合物具有出色的TGFβ抑制活性。
• Quinoline and quinazoline derivatives inhibiting platelet-derived growth
  申请人：Kirin Beer Kabushiki Kaisha

  公开号：US06143764A1

  公开（公告）日：2000-11-07

  The present invention relates to novel quinoline derivatives and quinazoline derivatives represented by the following formula (I): ##STR1## [wherein R.sub.1 and R.sub.2 are each independently H or C.sub.1 -C.sub.4 -alkyl, or R.sub.1 and R.sub.2 together form C.sub.1 -C.sub.3 -alkylene, X is O, S or CH.sub.2, W is CH or N, and Q is a substituted aryl group or substituted heteroaryl group] and their pharmaceutically acceptable salts, having platelet-derived growth factor receptor autophosphorylation inhibitory activity, to pharmaceutical compositions containing these compounds, and to methods for the treatment of diseases associated with abnormal cell growth such as tumors.

  本发明涉及一种新型喹啉衍生物和喹嗪衍生物，其由以下式子（I）所表示：##STR1## [其中R.sub.1和R.sub.2各自独立地为H或C.sub.1-C.sub.4-烷基，或者R.sub.1和R.sub.2共同形成C.sub.1-C.sub.3-亚烷基，X为O、S或CH.sub.2，W为CH或N，Q为取代芳基或取代杂环芳基]及其药学上可接受的盐，具有血小板源性生长因子受体自磷酸化抑制活性，以及含有这些化合物的制药组合物，以及用于治疗与异常细胞生长相关的疾病，如肿瘤的方法。
• COMPOUND HAVING TGFBETA INHIBITORY ACTIVITY AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
  申请人：Shimizu Kiyoshi

  公开号：US20090312313A1

  公开（公告）日：2009-12-17

  The present invention provides compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein X represents CH or N; Z represents —O—, —NH— or —C(═O)—; R and R′ represent a hydrogen atom, hydroxyl, a halogen atom, optionally substituted alkyl, optionally substituted alkenyl optionally substituted alkoxy, amino, aminocarbonyl, or an optionally substituted heterocyclic group; and A represents an optionally substituted specific carbocyclic or heterocyclic group. The compounds according to the present invention have excellent TGFβ inhibitory activity.

  本发明提供了由式(I)表示的化合物及其药学上可接受的盐和溶剂： 其中，X代表CH或N；Z代表—O—、—NH—或—C(═O)—；R和R′代表氢原子、羟基、卤素原子、可选取代的烷基、可选取代的烯基、可选取代的烷氧基、氨基、氨基甲酰基或可选取代的杂环基；A代表可选取代的特定环烷基或杂环基。本发明的化合物具有优异的TGFβ抑制活性。