8-甲氧基-1-甲基-2(1H)-喹啉酮 | 60443-14-3

• 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: 8-甲氧基-1-甲基-2(1H)-喹啉酮
• 英文名称: 8-methoxy-1-methylquinolin-2(1H)-one
• 英文别名: 8-methoxy-1-methyl-2-quinolone；8-methoxy-1-methylcarbostyril；8-methoxy-1-methyl-1H-quinolin-2-one；8-Methoxy-1-methyl-1H-chinolin-2-on；1-methyl-8-(methyloxy)-2(1H)-quinolinone；8-methoxy-1-methyl-1H-quinolin-2-one；8-methoxy-1-methylquinolin-2-one
• CAS: 60443-14-3
• 化学式: C₁₁H₁₁NO₂
• mdl: MFCD02926569
• 分子量: 189.214
• InChiKey: AVXUIKMMJRWEIW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.181
• 拓扑面积：
  29.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  8-甲氧基-1-甲基-2(1H)-喹啉酮 在 水 作用下， 以 氢溴酸 、 溶剂黄146 为溶剂， 反应 7.0h， 以afforded a white solid (2.0 g, 82%)的产率得到1-甲基-8-羟基-2-喹诺酮
  参考文献：
  名称：

  Substituted 1-Methyl-1H-Quinolin-2-Ones And 1-Methyl-1H-1,5-Naphthyridin-2-Ones As Antibacterials

  摘要：

  双环氮含有化合物及其作为抗菌剂的用途。

  公开号：

  US20100256124A1
• 作为产物：
  描述：

  N-methyl, 8-methoxy quinolinium iodide 在 氢氧化钾 、 potassium hexacyanoferrate(III) 作用下， 以 乙醚 、 水 为溶剂， 以40%的产率得到8-甲氧基-1-甲基-2(1H)-喹啉酮
  参考文献：
  名称：

  Gesto, C.; Cuesta, E. de la; Avendano, C., Synthetic Communications, 1990, vol. 20, # 1, p. 35 - 39

  摘要：

  DOI：

文献信息

• An organocatalyst bound α-aminoalkyl radical intermediate for controlled aerobic oxidation of iminium ions
  作者：Abdul Motaleb、Asish Bera、Pradip Maity

  DOI：10.1039/c8ob01032c

  日期：——

  A catalyst bound α-aminoalkyl radical intermediate from iminium is developed to control its formation and reactivity with aerobic oxygen. The influence of the catalyst was demonstrated via the ease of radical intermediate formation and its subsequent reactivity, including the first catalyst-controlled enantioselective aerobic oxidation with a chiral phosphite catalyst.

  研发了一种由催化剂与催化剂结合的亚胺基α-氨基烷基自由基中间体，以控制其形成和与好氧的反应性。通过容易形成自由基中间体及其随后的反应性证明了催化剂的影响，包括使用手性亚磷酸酯催化剂进行的第一催化剂控制的对映选择性好氧氧化反应。
• [EN] CARBOSTYRIL COMPOUND<br/>[FR] DÉRIVÉ DE CARBOSTYRILE
  申请人：OTSUKA PHARMA CO LTD

  公开号：WO2006035954A1

  公开（公告）日：2006-04-06

  The present invention provides a carbostyril compound represented by General Formula (1) or a salt thereof, wherein A is a direct bond, a lower alkylene group, or a lower alkylidene group; X is an oxygen atom or a sulfur atom; R4 and R5 each represent a hydrogen atom; the bond between the 3 and 4 positions of the carbostyril skeleton is a single bond or a double bond; R1 is a hydrogen atom, etc; R2 is a hydrogen atom, etc; and R3 is a hydrogen atom, etc. The carbostyril compound or salt thereof of the present invention induces the production of TFF, and thus is usable for the treatment and/or prevention of disorders such as alimentary tract diseases, oral diseases, upper respiratory tract diseases, respiratory tract diseases, eye diseases, cancers, and wounds.

  本发明提供了一种由通式（1）表示的羧基吲哚化合物或其盐，其中A是直链键、较低的烷基烯基或较低的烷基亚烯基；X是氧原子或硫原子；R4和R5分别表示氢原子；羧基吲哚骨架的3和4位置之间的键是单键或双键；R1是氢原子，等等；R2是氢原子，等等；R3是氢原子，等等。本发明的羧基吲哚化合物或其盐诱导TFF的产生，因此可用于治疗和/或预防消化道疾病、口腔疾病、上呼吸道疾病、呼吸道疾病、眼部疾病、癌症和伤口等疾病。
• Synthesis of Methoxy-2-quinolones via Pummerer-type Cyclization of N-Aryl-N-methyl-3-(phenylsulfinyl)propionamides.
  作者：Jun TODA、Michiya SAKAGAMI、Yoko GOAN、Mina SIMAKATA、Toshiaki SAITOH、Yoshie HORIGUCHI、Takehiro SANO

  DOI：10.1248/cpb.48.1854

  日期：——

  The thionium ions 10 generated by Pummerer reaction of N-aryl-N-methyl-3-(phenylsulfinyl)propionamides 4 caused not only an electrophilic cyclization reaction producing 2-quinolones 8, but also the formation of the vinyl sulfides 5 and 6 in favor of the latter reaction. On the other hand, the treatment of the vinyl sulfides 5 and 6 with p-toluenesulfonic acid induced cyclization to afford the 2-quinolones

  由N-芳基-N-甲基-3-（苯基亚磺酰基）丙酰胺Pummerer反应产生的硫鎓离子10不仅引起产生2-喹诺酮8的亲电环化反应，而且有利地形成了乙烯基硫化物5和6。后一种反应。另一方面，取决于芳环的电子性质，用对甲苯磺酸对乙烯基硫化物5和6的处理引起环化，从而以优异至中等的收率得到2-喹诺酮8，从而提供了一种方便的方法用于合成甲氧基-2-喹诺酮。
• 5-[1-Hydroxy-2-(substituted-amino)]alkyl-8-substituted-carbostyril and
  申请人：Otsuka Pharmaceutical Company Limited

  公开号：US04022784A1

  公开（公告）日：1977-05-10

  5-[1-Hydroxy-2-(substituted-amino)]alkyl-8-substituted-carbostyril derivatives and 5-[1-hydroxy-2-(substituted-amino)]-alkyl-8-substituted-3,4-dihydrocarbost yril derivatives represented by the formulas (Ia) and (Ib) ##STR1## WHEREIN R.sup.1, R.sup.4 and R.sup.5 each represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, with at least one of R.sup.4 and R.sup.5 being an alkyl group, and R.sup.2 and R.sup.3, which may be the same or different, each represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an aralkyl group containing a straight or branched chain alkyl moiety having 1 to 4 carbon atoms or a cycloalkyl group having 4 to 6 carbon atoms, or R.sup.2 and R.sup.3 may, when taken together with the nitrogen atom to which they are attached, form a 5- or 6-membered substituted or unsubstituted heterocyclic ring containing 1 or 2 nitrogen, oxygen or sulfur atoms as hetero atoms, the pharmaceutically acceptable acid addition salts thereof, and a process for preparing the same.

  5-[1-羟基-2-(取代氨基)]烷基-8-取代-碳基喹啉衍生物和5-[1-羟基-2-(取代氨基)]-烷基-8-取代-3,4-二氢碳基喹啉衍生物由以下式(Ia)和(Ib)所表示：其中R.sup.1、R.sup.4和R.sup.5分别代表氢原子或具有1至4个碳原子的烷基基团，其中至少一个为烷基基团，而R.sup.2和R.sup.3，可以相同也可以不同，分别代表氢原子、具有1至4个碳原子的烷基基团、包含具有1至4个碳原子的直链或支链烷基基团的芳基烷基基团或具有4至6个碳原子的环烷基基团，或者R.sup.2和R.sup.3可以与它们连接的氮原子一起形成一个含有1或2个氮、氧或硫原子作为杂原子的5-或6-成员取代或未取代杂环的环，以及其药学上可接受的酸盐和制备方法。
• Carbostyril compound
  申请人：Kuroda Takeshi

  公开号：US20070179173A1

  公开（公告）日：2007-08-02

  The present invention provides a carbostyril compound represented by General Formula (1) or a salt thereof, wherein A is a direct bond, a lower alkylene group, or a lower alkylidene group; X is an oxygen atom or a sulfur atom; R 4 and R 5 each represent a hydrogen atom; the bond between the 3 and 4 positions of the carbostyril skeleton is a single bond or a double bond; R 1 is a hydrogen atom, etc; R 2 is a hydrogen atom, etc; and R 3 is a hydrogen atom, etc. The carbostyril compound or salt thereof of the present invention induces the production of TFF, and thus is usable for the treatment and/or prevention of disorders such as alimentary tract diseases, oral diseases, upper respiratory tract diseases, respiratory tract diseases, eye diseases, cancers, and wounds.

  本发明提供了一种由通式（1）表示的碳基噻吩化合物或其盐，其中A是直接键，较低的烷基烷基或较低的烷基亚烷基；X是氧原子或硫原子；R4和R5分别表示氢原子；碳基噻吩骨架的3和4位之间的键是单键或双键；R1是氢原子等；R2是氢原子等；R3是氢原子等。本发明的碳基噻吩化合物或其盐能够诱导TFF的产生，因此可用于治疗和/或预防消化道疾病、口腔疾病、上呼吸道疾病、呼吸道疾病、眼部疾病、癌症和伤口等疾病。