6-羟基-1-甲基-3,4-二氢喹啉-2-酮 | 69601-46-3

• 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
• 中文名称: 6-羟基-1-甲基-3,4-二氢喹啉-2-酮
• 英文名称: 6-hydroxy-1-methyl-3,4-dihydroquinolin-2(1H)-one
• 英文别名: 6-Hydroxy-1-methyl-2-oxo-1,2,3,4-tetrahydroquinoline；6-hydroxy-1-methyl-3,4-dihydroquinolin-2-one
• CAS: 69601-46-3
• 化学式: C₁₀H₁₁NO₂
• 分子量: 177.203
• InChiKey: XCXDDKNPUFGHKD-UHFFFAOYSA-N

物化性质

• 沸点：
  478.1±45.0 °C(Predicted)
• 密度：
  1.245±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  13
• 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：
  40.5
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 海关编码：
  2933790090

反应信息

• 作为反应物：
  描述：

  2-碘代丙烷 、 6-羟基-1-甲基-3,4-二氢喹啉-2-酮 在 caesium carbonate 作用下， 以 丙酮 为溶剂， 生成 6-isopropoxy-1-methyl-2-oxo-1,2,3,4-tetrahydroquinoline
  参考文献：
  名称：

  Substituted benzolactam compounds

  摘要：

  这项发明涉及通式（1）：1的化合物或其药学上可接受的盐，其中W、T、Y、X、Q、R1、R2和R3的定义如本文所述。本发明还涉及上述示出的通式I的化合物，其中Y为—NH—；T为（2S,3S）-2-苯基哌啶-3-基，其中所述（2S,3S）-2-苯基哌啶-3-基的苯基可以选择地被氟取代；Q为氧并与其连接的碳原子双键结合，X为甲氧基或乙氧基，R1为氢、甲基或卤代-C1-C2烷基，W为亚甲基、乙烯基或乙烯基；R2和R3独立地为氢或甲基，或R2或R3中的一个可能为羟基，当W为乙烯基时，R2和R3均为甲基，当W为亚甲基时，R2和R3均为氢，当W为乙烯基时，R2和R3均为氢。该发明进一步涉及使用上述化合物及其药物组成物治疗各种中枢神经系统和其他疾病的方法。

  公开号：

  US20030105124A1
• 作为产物：
  描述：

  6-甲氧基-1-甲基-1,2,3,4-四氢喹啉-2-酮 在 三溴化硼 作用下， 以 二氯甲烷 为溶剂， 生成 6-羟基-1-甲基-3,4-二氢喹啉-2-酮
  参考文献：
  名称：

  [EN] APOL1 INHIBITORS AND METHODS OF USE
  [FR] INHIBITEURS D'APOL1 ET MÉTHODES D'UTILISATION

  摘要：

  Provided herein are compounds of formula (II): or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, whereinm, n, p, R1, R2, R3, L1, L2, L3, R4, X1, X2, X3, and X4are as defined herein. Also provided are methods of preparing compounds of formula (II), or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing. Also provided are methods of inhibiting APOL1 and methods of treating an APOL1 -mediated disease, disorder, or condition in an individual.

  公开号：

  WO2023141432A2

文献信息

• Benzoamide piperidine containing compounds and related compounds
  申请人：——

  公开号：US20030087925A1

  公开（公告）日：2003-05-08

  The present invention relates to certain benzoamide piperidine containing compounds and related compounds that exhibit activity as NK-1 receptor antagonists, (e.g., substance P receptor antagonists), to pharmaceutical compositions containing them, and to their use in the treatment and prevention of central nervous system disorders, inflammatory disorders, cardiovascular disorders, ophthalmic disorders, gastrointestinal disorders, disorders caused by helicobacter pylori, disorders of the immune system, urinary incontinence, pain, migraine, emesis, angiogenesis and other disorders.

  本发明涉及某些含有苯甲酰胺哌啶类化合物和相关化合物，这些化合物表现出作为NK-1受体拮抗剂（例如，物质P受体拮抗剂）的活性，以及含有它们的药物组合物，以及它们在治疗和预防中枢神经系统疾病、炎症性疾病、心血管疾病、眼科疾病、消化系统疾病、幽门螺杆菌引起的疾病、免疫系统疾病、尿失禁、疼痛、偏头痛、呕吐、血管生成和其他疾病的治疗中的用途。
• Substituted benzolactam compounds
  申请人：——

  公开号：US20030105124A1

  公开（公告）日：2003-06-05

  This invention relates to compounds of the general formula (1): 1 or a pharmaceutically acceptable salt thereof, W, T, Y, X, Q, R 1 , R 2 , and R 3 are defined herein. This invention also relates to compounds of the formula I, depicted above, wherein Y is —NH—; T is (2S,3S)-2-phenylpiperidin-3-yl, where the phenyl group of said (2S, 3S)-2-phenylpiperidine-3-yl may optionally be substituted with fluoro; Q is oxygen and is double bonded to the carbon atom to which it is attached, X is methoxy or ethoxy, R 1 is hydrogen, methyl or halo-C 1 -C 2 alkyl, W is methylene, ethylene or vinylene; R 2 and R 3 are independently hydrogen or methyl, or one of R 2 or R 3 may be hydroxy, when W is ethylene, R 2 and R 3 are both methyl, when W is methylene, and R 2 and R 3 are both hydrogen, when W is vinylene. The invention is further directed to methods of treating various CNS and other disorders using said compounds and pharmaceutical compositions thereof.

  这项发明涉及通式（1）：1的化合物或其药学上可接受的盐，其中W、T、Y、X、Q、R1、R2和R3的定义如本文所述。本发明还涉及上述示出的通式I的化合物，其中Y为—NH—；T为（2S,3S）-2-苯基哌啶-3-基，其中所述（2S,3S）-2-苯基哌啶-3-基的苯基可以选择地被氟取代；Q为氧并与其连接的碳原子双键结合，X为甲氧基或乙氧基，R1为氢、甲基或卤代-C1-C2烷基，W为亚甲基、乙烯基或乙烯基；R2和R3独立地为氢或甲基，或R2或R3中的一个可能为羟基，当W为乙烯基时，R2和R3均为甲基，当W为亚甲基时，R2和R3均为氢，当W为乙烯基时，R2和R3均为氢。该发明进一步涉及使用上述化合物及其药物组成物治疗各种中枢神经系统和其他疾病的方法。
• Novel carbostyril derivatives
  申请人：Otsuka Pharmaceutical Co., Ltd.

  公开号：US04298739A1

  公开（公告）日：1981-11-03

  Novel carbostyril derivatives having platelet aggregation inhibitory action, antiinflamatory action, antiulcer action, vasodilatory action and phosphodiesterase inhibitory action and are useful for preventing or curing thrombus, arteriosclerosis, hypertension, asthma and other like diseases, and also useful as an antiinflamatory or anti-ulcer agent, represented by the formula ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, phenyl-C.sub.1-4 alkyl-; R.sup.2 is hydrogen, a halogen atom, hydroxy, phenyl-C.sub.1-4 alkoxy; R.sup.3 is hydrogen, hydroxy, C.sub.1-4 alkyl; R.sup.4 is C.sub.3-8 cycloalkyl, substituted or unsubstituted phenyl, C.sub.3-8 cycloalkyl-C.sub.1-4 alkyl, 2-(3,4-dimethoxyphenyl)-ethyl, R.sup.5 is hydrogen, C.sub.1-8 alkyl, C.sub.2-4 alkenyl, phenyl, C.sub.3-8 cycloalkyl, phenyl-C.sub.1-4 alkyl, C.sub.3-8 cycloalkyl-C.sub.1-4 alkyl, m is an integer of 1 - 3, l and n which may be same or different, and are respectively 0 or an integer of 1 - 7 and the sum of l and n is not exceeding 7, the carbon-carbon bond at 3- and 4-positions in the carbostyril skelton is either single or double bond.

  具有血小板聚集抑制作用、抗炎作用、抗溃疡作用、扩血管作用和磷酸二酯酶抑制作用的新型羧甲基苯基吡咯衍生物，可用于预防或治疗血栓、动脉硬化、高血压、哮喘等疾病，并可用作抗炎或抗溃疡剂，其化学式表示为：##STR1## 其中，R1为氢、C1-4烷基、C2-4烯基、苯基-C1-4烷基；R2为氢、卤素原子、羟基、苯基-C1-4烷氧基；R3为氢、羟基、C1-4烷基；R4为C3-8环烷基、取代或未取代苯基、C3-8环烷基-C1-4烷基、2-(3,4-二甲氧基苯基)-乙基、R5为氢、C1-8烷基、C2-4烯基、苯基、C3-8环烷基、苯基-C1-4烷基、C3-8环烷基-C1-4烷基，m为1-3的整数，l和n可以相同或不同，分别为0或1-7的整数，l和n的和不超过7，羧甲基苯基吡咯骨架的3-和4-位碳-碳键为单键或双键。
• Discovery of a Thioxanthone–TfOH Complex as a Photoredox Catalyst for Hydrogenation of Alkenes Using <i>p</i> ‐Xylene as both Electron and Hydrogen Sources
  作者：Wen‐Jie Kang、Bo Li、Meng Duan、Guangxing Pan、Weiqiang Sun、Aishun Ding、Yanbin Zhang、K. N. Houk、Hao Guo

  DOI：10.1002/anie.202211562

  日期：2022.11.25

  novel organic photoredox catalyst was discovered by simply adding a catalytic amount of TfOH as a co-catalyst to readily available thioxanthone. The new catalyst, 9-HTXTF, shows a sufficiently long singlet lifetime and adequately strong oxidation potential, as well as relatively facile photoexcitation, with applications in the hydrogenation and deuteration of carbonylated alkenes.

  通过简单地将催化量的 TfOH 作为助催化剂添加到容易获得的噻吨酮中，发现了一种新型有机光氧化还原催化剂。新型催化剂9-HTXTF具有足够长的单线态寿命和足够强的氧化电位，以及相对容易的光激发，可用于羰基化烯烃的氢化和氘化。
• Substituted benzolactam compounds as substance p antagonists
  申请人：——

  公开号：US20020052503A1

  公开（公告）日：2002-05-02

  This invention provides a compound of general formula (I) 1 and its pharmaceutically acceptable salts, wherein: W is methylene, ethylene, propylene, vinylene, —CH 2 —O—, —O—CH 2 —, —CO 2 —S— or —S—CH 2 —; R 1 , R 2 and R 3 are independently hydrogen, C 1 -C 3 alkyl, C 1 -C 3 alkoxy or halo C 1 -C 3 alkyl, provided that when W is methylene, both R 2 and R 3 are not hydrogen; X is halo, C 1 -C 3 alkoxy, C 1 -C 3 alkyl, halo C 1 -C 3 alkoxy or C 1 -C 3 alkenyl; Y is imino or oxy; Q is oxygen or sulfur; and T is (2S,3S)-2-diphenylmethylquinuclidin-3-yl, (2S,3S)-2-phenylpiperidin-3-yl or (2S,3S)-2-diphenylmethyl-1-azanorbornan-3-yl. These compounds are useful in the treatment of treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases, emesis, urinary incontinence, pain, migraine, angiogenesis or the like in a mammalian subject, especially humans. Also, intermediates of the above compounds are disclosed.

  本发明提供了通式 (I) 的化合物 1 及其药学上可接受的盐类，其中W 是亚甲基、乙烯、丙烯、乙烯基、-CH 2 -O-、-O-CH 2 -、-CO 2 -S-或-S-CH 2 -; R 1 , R 2 和 R 3 独立地为氢、C 1 -C 3 烷基 1 -C 3 烷氧基或卤代 C 1 -C 3 烷基，条件是当 W 为亚甲基时，两个 R 2 和 R 3 都不是氢；X 是卤代、C 1 -C 3 烷氧基 1 -C 3 烷基、卤代 C 1 -C 3 烷氧基或 C 1 -C 3 烯基；Y 是亚氨基或氧基；Q 是氧或硫；T 是 (2S,3S)-2-二苯甲基喹吖啶-3-基、(2S,3S)-2-苯基哌啶-3-基或 (2S,3S)-2-二苯甲基-1-氮杂降冰片烷-3-基。这些化合物可用于治疗哺乳动物，尤其是人类的胃肠道疾病、中枢神经系统疾病、炎症性疾病、呕吐、尿失禁、疼痛、偏头痛、血管生成或类似疾病。此外，还公开了上述化合物的中间体。