7-Methyl-3,4-dihydro-quinolin-2-ol | 19352-59-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 7-Methyl-3,4-dihydro-quinolin-2-ol
• CAS: 19352-59-1
• 化学式: C₁₀H₁₁NO
• mdl: MFCD13179105
• 分子量: 161.2
• InChiKey: IHVQLIWZGXUWFD-UHFFFAOYSA-N

物化性质

• 熔点：
  131 °C
• 沸点：
  332.6±41.0 °C(Predicted)
• 密度：
  1.111±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  1

安全信息

• 海关编码：
  2933790090

反应信息

• 作为反应物：
  描述：

  3,4-二氯苯甲酰氯 、 7-Methyl-3,4-dihydro-quinolin-2-ol 生成 3-[2-(3,4-Dichloro-benzoylamino)-4-methyl-phenyl]-propionic acid
  参考文献：
  名称：

  Anti-inflammatory properties of a series of phenyl- and phenoxy-alkanoic acids

  摘要：

  摘要：已合成一些o-苯甲酰基苯氧乙酸、苯基烷酸和苯氧烷酸。通过小鼠苯基苯醌扭曲实验和大鼠足部水肿实验测量了抗炎活性。苯甲酰环中的间位和对位取代，促进了脂溶性，增强了效力，而用极性基团取代则降低了效力。在2-(3,4-二氯苯甲酰胺)苯氧乙酸中进一步取代苯环仅稍微影响了效力。侧链修饰并未增加所选的三种取代苯氧乙酸的活性。两种苯丙酸显示出良好的活性顺序，但相应的肉桂酸几乎无活性。从研究中选择了2-(3,4-二氯苯甲酰胺)苯氧乙酸（SNR. 1804）进行进一步研究，目前正在进行临床评估。

  DOI：

  10.1111/j.2042-7158.1970.tb12754.x

文献信息

• INDANYLOXYDIHYDROBENZOFURANYLACETIC ACIDS
  申请人：ECKHARDT Matthias

  公开号：US20140163025A1

  公开（公告）日：2014-06-12

  The present invention relates to compounds of general formula I, wherein the groups (Het)Ar and R 1 are defined as in claim 1 , which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.

  本发明涉及一般式I的化合物， 其中基团(Het)Ar和R1如权利要求1所定义， 具有有价值的药理特性，特别是结合GPR40受体并调节其活性。这些化合物适用于治疗和预防可以受到该受体影响的疾病，如代谢性疾病，特别是2型糖尿病。
• THERAPEUTIC AGENT FOR CEREBRAL INFARCTION
  申请人：Nakao Akira

  公开号：US20120196824A1

  公开（公告）日：2012-08-02

  The invention provides a therapeutic drug for ischemic stroke. The therapeutic drug has the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof, as an active ingredient.

  这项发明提供了一种用于缺血性中风的治疗药物。该治疗药物具有如下式（I）的化学式，其中每个符号如本文所定义，或其药理学上可接受的盐，或其溶剂化物，作为活性成分。
• [EN] BENZOTHIADIAZINE COMPOUNDS<br/>[FR] COMPOSÉS BENZOTHIADIAZINE
  申请人：GLAXOSMITHKLINE IP DEV LTD

  公开号：WO2017098421A1

  公开（公告）日：2017-06-15

  The invention is directed to substituted benzothiadiazine derivatives. Specifically, the invention is directed to compounds according to Formula (I):wherein R, R1, R2, R3, R4 and R5 are as defined herein. The compounds of the invention are inhibitors of CD73 and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with CD73 inhibition, such as AIDS, autoimmune diseases, infections, atherosclerosis, and ischemia-reperfusion injury. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CD73 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

  本发明涉及取代苯并噻二嗪衍生物。具体而言，本发明涉及式(I)化合物：其中R、R1、R2、R3、R4和R5定义如下。本发明的化合物是CD73的抑制剂，可用于治疗癌症、前癌综合症和与CD73抑制相关的疾病，如艾滋病、自身免疫病、感染、动脉粥样硬化和缺血-再灌注损伤。因此，本发明进一步涉及包含本发明化合物的药物组合物。本发明更进一步的涉及使用本发明化合物或包含本发明化合物的药物组合物抑制CD73活性和治疗相关疾病的方法。
• Multibond Forming Tandem Reactions of Anilines via Stable Aryl Diazonium Salts: One-Pot Synthesis of 3,4-Dihydroquinolin-2-ones
  作者：Réka J. Faggyas、Megan Grace、Lewis Williams、Andrew Sutherland

  DOI：10.1021/acs.joc.8b01910

  日期：2018.10.19

  A fast and effective one-pot tandem process that generates Heck coupled products from readily available anilines via stable aryl diazonium tosylate salts was developed. The mild and simple procedure involves rapid formation of aryl diazonium salts using a polymer-supported nitrite reagent and p-tosic acid, followed by a base-free Heck–Matsuda coupling with acrylates and styrenes. Using 2-nitroanilines

  开发了一种快速有效的一锅串联方法，该方法可通过稳定的芳基重氮甲苯磺酸盐从易于获得的苯胺生成Heck偶联产物。温和而简单的步骤涉及使用聚合物负载的亚硝酸盐试剂和对羟基苯甲酸酯快速形成芳基重氮盐-甲苯磺酸，然后与丙烯酸酯和苯乙烯进行无碱Heck-Matsuda偶联。使用2-硝基苯胺作为底物，将一锅串联方法扩展到直接合成3,4-二氢喹啉-2-酮。在这种情况下，经过重氮化和Heck-Matsuda偶联生成肉桂酸甲酯，添加氢气并再利用钯催化剂还原硝基和烯烃氢化，可有效形成3,4-二氢喹啉-2-酮。 。一锅四步法的合成效用通过基于喹啉酮的钠离子通道调节剂的五锅法合成得到了证明。
• Methods for treating neisseria gonorrhoeae infection with substituted 1,2-dihydro-2A,5,8A-triazaacenaphthylene-3,8-diones
  申请人：GlaxoSmithKline Intellectual Property Development Limited

  公开号：US10702521B2

  公开（公告）日：2020-07-07

  The present invention relates to methods for treating Neisseria Gonorrhoeae infection which comprises administering to a subject in need thereof novel 1,2-dihydro-2a,5,8a-triazaacenaphthylene-3,8-dione compounds: or pharmaceutically acceptable salts thereof and/or corresponding pharmaceutical compositions.

  本发明涉及治疗淋病双球菌感染的方法，包括向需要的受试者施用新型1,2-二氢-2a,5,8a-三氮杂蒽-3,8-二酮化合物：或其药学上可接受的盐和/或相应的药物组合物。