(R)-4-((R)-1-(7-(3,4,5-trimethoxyphenyl)quinolin-5-yloxy)ethyl)pyrrolidin-2-one | 1421339-71-0

• 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: (R)-4-((R)-1-(7-(3,4,5-trimethoxyphenyl)quinolin-5-yloxy)ethyl)pyrrolidin-2-one
• 英文别名: (4R)-4-[(1R)-1-[7-(3,4,5-trimethoxyphenyl)quinolin-5-yl]oxyethyl]pyrrolidin-2-one
• CAS: 1421339-71-0
• 化学式: C₂₄H₂₆N₂O₅
• 分子量: 422.481
• InChiKey: BNPMNIBMJDEQFP-RHSMWYFYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  31
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  78.9
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  (R)-N-methoxy-N-methyl-5-oxo-1-((R)-1-phenylethyl)pyrrolidine-3-carboxamide 在 偶氮二甲酸二叔丁酯 、 三苯基膦 、 lithium dihydrido borata-bicyclo[3.3.0]nonane 作用下， 以 四氢呋喃 、 乙醚 、 二氯甲烷 为溶剂， 反应 10.5h， 生成 (R)-4-((R)-1-(7-(3,4,5-trimethoxyphenyl)quinolin-5-yloxy)ethyl)pyrrolidin-2-one
  参考文献：
  名称：

  Substituted Quinolines and Their Use As Medicaments

  摘要：

  揭示了公式1的取代喹啉，其中R1和R2在此处定义，以及制备和使用它们的方法。

  公开号：

  US20130029949A1

文献信息

• [EN] SUBSTITUTED QUINOLINES AND THEIR USE AS MEDICAMENTS<br/>[FR] QUINOLÉINES SUBSTITUÉES ET LEUR UTILISATION COMME MÉDICAMENTS
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2013014060A1

  公开（公告）日：2013-01-31

  The invention relates to new substituted quinolines of formula (1) wherein R1 is a linear or branched C1-6-alkyl, wherein R1 may optionally be substituted by R3 which is selected from the group consisting of a three-, four-, five-, six- or seven-membered cycloalkl; a five-, six- or seven-membered, saturated heterocycle comprising one, two or three heteroatoms each independently selected from the group consisting of N, S and O; and a five- or six-membered heteroaryl comprising one, two or three heteroatoms each independently selected from the group consisting of N, S and O; wherein R3 may optionally be substituted further substituted as defined in claim 1 and wherein R2 is selected from the group consisting of halogen, phenyl, a five- or six-membered monocyclic heteroaryl comprising one, two or three heteroatoms each independently selected from the group consisting of N, S and O; a bicyclic, nine-, ten- or eleven-membered, either aromatic or non-aromatic, but not fully saturated heterocycle comprising one, two, three or four heteroatoms each independently selected from the group consisting of N, S and O; wherein R2 may optionally be further substituted as defined in claim 1, and their use in the preparation of medicaments for the treatment of disease such as asthma, COPD, allergic rhinitis, allergic dermatitis and rheumatoid arthritis.

  该发明涉及公式（1）中的新取代喹啉，其中R1是直链或支链的C1-6-烷基，其中R1可以选择性地被R3取代，R3选自以下组：三、四、五、六或七元环烷基；含有一个、两个或三个异原子（分别独立地选自N、S和O）的五、六或七元饱和杂环；含有一个、两个或三个异原子（分别独立地选自N、S和O）的五元或六元杂芳基；其中R3可以选择性地进一步取代，如权利要求书中所定义，R2选自以下组：卤素、苯基、含有一个、两个或三个异原子（分别独立地选自N、S和O）的五元或六元单环杂芳基；含有一个、两个、三或四个异原子（分别独立地选自N、S和O）的九、十或十一元双环芳香或非芳香但不完全饱和杂环；其中R2可以选择性地进一步取代，如权利要求书中所定义，并且它们在制备用于治疗哮喘、慢性阻塞性肺病、过敏性鼻炎、过敏性皮炎和类风湿性关节炎等疾病的药物中的用途。
• Substituted quinolines and their use as medicaments
  申请人：Hoffmann Matthias

  公开号：US08912173B2

  公开（公告）日：2014-12-16

  Disclosed are substituted quinolines of formula 1 wherein R1 and R2 are defined herein, the processing of making and using the same.

  本发明涉及公式1中的取代喹啉，其中R1和R2在此定义，以及其制备和使用方法。
• HETEROARYL SYK INHIBITORS
  申请人：BOEHRINGER INGELHEIM INTERNATIONAL GMBH

  公开号：US20160244446A1

  公开（公告）日：2016-08-25

  The invention relates to new substituted heteroaryls of formula (1), wherein A is selected from the group consisting of N and CH, D is CH, E is selected from the group consisting of C and N, T is C, G is selected from the group consisting of C and N, and wherein each of the broken (dotted) double bonds in ring 1 are selected from either a single bond or a double bond under the proviso that all single and double bonds of ring 1 are arranged in such a way that they all form together with ring 2 an aromatic ring system, and wherein R 1 , M and R 3 are defined according to claim 1 , and to the above compounds for the treatment of a disease selected from the group consisting of asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes, lupus nephritis and rheumatoid arthritis.

  本发明涉及一种新的式子（1）的取代杂环芳基，其中A选择自N和CH组成的群体，D为CH，E选择自C和N组成的群体，T为C，G选择自C和N组成的群体，其中在环1中的所有破碎（虚线）双键选择为单键或双键，前提是环1的所有单键和双键排列在一起，与环2一起形成一个芳香环系统，其中R1、M和R3根据权利要求所定义，以及上述化合物用于治疗哮喘、COPD、过敏性鼻炎、过敏性皮炎、红斑狼疮、狼疮性肾炎和类风湿性关节炎等疾病。
• Heteroaryl SYK inhibitors
  申请人：Boehringer Ingelheim International GmbH

  公开号：US10947243B2

  公开（公告）日：2021-03-16

  The invention relates to new substituted heteroaryls of formula 1 wherein A is selected from the group consisting of N and CH D is selected from the group consisting of CH, N, NH, S and O, E is selected from the group consisting of C and N, T is selected from the group consisting of C and N, G is selected from the group consisting of C and N, and wherein each of the broken (dotted) double bonds in ring 1 are selected from either a single bond or a double bond under the proviso that all single and double bonds of ring 1 are arranged in such a way that they all form together with ring 2 an aromatic ring system, and wherein R1, M and R3 are defined according to claim 1, and to the above compounds for the treatment of a disease selected from the group consisting of asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes, lupus nephritis and rheumatoid arthritis.

  本发明涉及式 1 的新取代杂芳基 其中 A 选自 N 和 CH 组成的组 D 选自 CH、N、NH、S 和 O 组成的组、 E 选自 C 和 N 组成的组、 T 选自 C 和 N 组成的组、 G 选自 C 和 N 组成的组、 其中环 1 中的每个断裂（点状）双键选自单键或双键，但条件是环 1 的所有单键和双键的排列方式使它们与环 2 一起形成一个芳香环系统、 其中 R1、M和R3根据权利要求1定义，上述化合物用于治疗选自哮喘、慢性阻塞性肺病、过敏性鼻炎、过敏性皮炎、红斑狼疮、狼疮性肾炎和类风湿性关节炎的疾病。
• SUBSTITUTED QUINOLINES AND THEIR USE AS MEDICAMENTS
  申请人：Boehringer Ingelheim International GmbH

  公开号：EP2736886A1

  公开（公告）日：2014-06-04