(3,4-二氯苯基)-(4-甲氧基苯基)甲酮 | 66938-32-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: (3,4-二氯苯基)-(4-甲氧基苯基)甲酮
• 英文名称: 3,4-dichlorophenyl 4-methoxyphenyl ketone
• 英文别名: 3,4-dichloro-4'-methoxybenzophenone；3,4-Dichlor-4'-methoxy-benzophenon；(3,4-dichlorophenyl)-(4-methoxyphenyl)methanone
• CAS: 66938-32-7
• 化学式: C₁₄H₁₀Cl₂O₂
• mdl: MFCD06201535
• 分子量: 281.138
• InChiKey: JFXBDLZCKLTJRY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.071
• 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：

  (3,4-二氯苯基)-(4-甲氧基苯基)甲酮 在 manganese(IV) oxide 、 magnesium sulfate 、 一水合肼 、 溶剂黄146 作用下， 以 乙醇 、 二氯甲烷 为溶剂， 反应 13.0h， 生成 1,2-dichloro-4-(diazo(4-methoxyphenyl)methyl)benzene
  参考文献：
  名称：

  铑催化的对映选择性 B-H 键插入 gem-二芳基卡宾：有效获取 gem-二芳基甲炔硼烷

  摘要：

  我们报告了以二芳基重氮甲烷作为卡宾前体的高对映选择性二铑催化的 B-H 键插入反应。这些反应以高产率（高达 99 % 的产率）、高活性（高达 14 300 的转化率）、高对映选择性（高达 99 % ee）提供了手性 gem-二芳基次甲基硼烷化合物，并显示出前所未有的广泛官能团耐受性。

  DOI：

  10.1002/anie.202109447
• 作为产物：
  描述：

  3,4-二氯苯甲醛 在 magnesium 、 2-碘酰基苯甲酸 作用下， 以 四氢呋喃 、 二甲基亚砜 、 1,2-二溴乙烷 为溶剂， 反应 6.0h， 生成 (3,4-二氯苯基)-(4-甲氧基苯基)甲酮
  参考文献：
  名称：

  铑催化的对映选择性 B-H 键插入 gem-二芳基卡宾：有效获取 gem-二芳基甲炔硼烷

  摘要：

  我们报告了以二芳基重氮甲烷作为卡宾前体的高对映选择性二铑催化的 B-H 键插入反应。这些反应以高产率（高达 99 % 的产率）、高活性（高达 14 300 的转化率）、高对映选择性（高达 99 % ee）提供了手性 gem-二芳基次甲基硼烷化合物，并显示出前所未有的广泛官能团耐受性。

  DOI：

  10.1002/anie.202109447

文献信息

• Synthesis and structure-activity relationships of benzophenone hydrazone derivatives with insecticidal activity
  作者：Manfred B�ger、Dieter D�rr、Laurenz Gsell、Roger G Hall、Friedrich Karrer、Odd Kristiansen、Peter Maienfisch、Alfons Pascual、Alfred Rindlisbacher

  DOI：10.1002/1526-4998(200102)57:2<191::aid-ps275>3.0.co;2-o

  日期：2001.2

  A broad range of benzophenone hydrazone derivatives was prepared and tested against selected chewing insect pests, allowing the analysis of structure-activity relationships. Good activity was found only when the aromatic rings were substituted at the 4-positions with an halogen atom and a triflate or perhaloalkoxy group. In contrast, a number of substituents on the hydrazone part led to active compounds

  制备了广泛的二苯甲酮衍生物，并针对选定的咀嚼害虫进行了测试，从而分析了结构-活性关系。仅当芳环在4-位被卤素原子和三氟甲磺酸酯或全卤代烷氧基取代时，才发现良好的活性。相反，部分上的许多取代基导致活性化合物，用酰基型取代基可获得最佳结果。在针对斜纹夜蛾的半田间试验中证实了最佳代表的出色的实验室和温室活性。
• 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.

  本发明涉及由以下式（I）表示的新型喹啉衍生物和喹唑啉衍生物：[其中R.sub.1和R.sub.2分别独立地为H或C.sub.1 -C.sub.4 -烷基，或R.sub.1和R.sub.2一起形成C.sub.1 -C.sub.3 -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芳基]及其在药学上可接受的盐，具有血小板源性生长因子受体自磷酸化抑制活性，用于含有这些化合物的药物组合物，以及用于治疗与异常细胞生长（如肿瘤）相关的疾病的方法。
• Lithiation of 2-Aryl-2-(chloroaryl)-1,3-dioxolanes and Its Application in the Synthesis of Newortho-Functionalized Benzophenone Derivatives
  作者：Gyula Lukács、Márta Porcs-Makkay、Gyula Simig

  DOI：10.1002/ejoc.200400335

  日期：2004.10

  2-Aryl-2-(chloroaryl)-1,3-dioxolanes 4 were lithiated ortho to the ketal group of the chloroaryl ring by treatment with butyllithium in THF between −78 and 0 °C. The site selectivity of some of the deprotonation reactions was rationalized by the long-range effect of the 4-chloro substituent. The lithio species thus generated were treated with various electrophiles to give ortho-functionalized benzophenone

  2-芳基-2-(氯芳基)-1,3-二氧戊环 4 通过在-78 和 0 °C 之间的 THF 中用丁基锂处理，在氯芳基环的缩酮基团的邻位锂化。一些去质子化反应的位点选择性通过 4-氯取代基的长程效应合理化。用各种亲电试剂处理由此产生的锂硫物质，得到邻位官能化的二苯甲酮衍生物。在 2-(4-氯苯基)-2-(4-氟苯基)-1,3-二氧戊环 (4s) 的锂化过程中观察到芳环之间的分子内竞争。(© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004)
• Synthesis and structure–activity relationship for new series of 4-Phenoxyquinoline derivatives as specific inhibitors of platelet-derived growth factor receptor tyrosine kinase
  作者：Kazuo Kubo、Shin-ichi Ohyama、Toshiyuki Shimizu、Atsuya Takami、Hideko Murooka、Tsuyoshi Nishitoba、Shinichiro Kato、Mikio Yagi、Yoshiko Kobayashi、Noriko Iinuma、Toshiyuki Isoe、Kazuhide Nakamura、Hiroshi Iijima、Tatsushi Osawa、Toshio Izawa

  DOI：10.1016/j.bmc.2003.08.020

  日期：2003.11

  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.
• Raeymackers; Van Gelder; Roevens, Arzneimittel-Forschung/Drug Research, 1978, vol. 28, # 4, p. 586 - 594
  作者：Raeymackers、Van Gelder、Roevens、Janssen

  DOI：——

  日期：——