6-bromo-2,4-dimethylquinazoline | 1806-65-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 6-bromo-2,4-dimethylquinazoline
• CAS: 1806-65-1
• 化学式: C₁₀H₉BrN₂
• 分子量: 237.099
• InChiKey: CKPBMNWUPCRVMC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  25.8
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  N-(2-乙酰基-4-溴苯基)乙酰胺 在 ammonium acetate 、 溶剂黄146 作用下， 反应 48.0h， 以90 mg的产率得到6-bromo-2,4-dimethylquinazoline
  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] AMINO QUINAZOLINE DERIVATIVES AS P2X3 INHIBITORS<br/>[FR] DÉRIVÉS D'AMINO QUINAZOLINE SERVANT D'INHIBITEURS DE P2X3
  申请人：CHIESI FARM SPA

  公开号：WO2020239951A1

  公开（公告）日：2020-12-03

  The present invention relates to compounds of formula I inhibiting P2X purinoceptor 3; particularly the invention relates to compounds that are amino quinazoline derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. The compounds of the invention may be useful in the treatment of many disorders associated with P2X3 receptors mechanisms, such as respiratory diseases including cough, asthma, idiopathic pulmonary fibrosis (IPF) and chronic obstructive pulmonary disease (COPD).

  本发明涉及抑制P2X嘌呤受体3的I式化合物；特别是涉及氨基喹唑啉衍生物的化合物，制备这种化合物的方法，含有它们的药物组合物以及它们的治疗用途。本发明的化合物可能在治疗与P2X3受体机制相关的许多疾病中有用，如呼吸道疾病，包括咳嗽、哮喘、特发性肺纤维化（IPF）和慢性阻塞性肺病（COPD）。
• [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。
• Mild synthesis of quinazolines from 2,2,2-trichloroethyl imidates and 2-aminophenyl ketones
  作者：Yanan Wu、Hongyi Zhao、Haihong Huang、Dongfeng Zhang

  DOI：10.1016/j.tetlet.2022.154313

  日期：2023.2

  metal-free method for the synthesis of quinazolines from 2-aminophenyl ketones and 2,2,2‑trichloroethyl imidates hydrochloride in the presence of sodium acetate is reported. The present approach has advantages including mild reaction conditions, readily available starting materials, and gram-scale synthesis. This methodology leads to an efficient construction of various quinazoline derivatives in moderate

  在此，报道了一种在乙酸钠存在下由 2-氨基苯基酮和 2,2,2-三氯亚胺酸乙酯盐酸盐合成喹唑啉的无金属方法。本方法具有反应条件温和、原料易得和克级合成等优点。这种方法导致以中等到高产率有效地构建各种喹唑啉衍生物。
• Visible-light photocatalyzed C–N bond activation of tertiary amines: a three-component approach to synthesize quinazolines
  作者：Ajithkumar Arumugam、Gopal Chandru Senadi

  DOI：10.1039/d3ob02067c

  日期：——

  three-component approach has been developed to prepare 2,4-disubstituted quinazolines from o-acylanilines, trialkylamines and ammonium chloride under visible-light using eosin Y as the photocatalyst. The notable features of this work include (i) the use of tertiary amines as an alkyl synthon and triethanolamine as a C2-OH synthon; (ii) good functional group tolerance with 52%–98% yields; (iii) proof of

  开发了一种无金属三组分方法，以曙红 Y 作为光催化剂，在可见光下由邻酰基苯胺、三烷基胺和氯化铵制备 2,4-二取代喹唑啉。这项工作的显着特点包括（i）使用叔胺作为烷基合成子和三乙醇胺作为C 2 -OH合成子； (ii) 良好的官能团耐受性，产率 52%–98%； (iii) 以邻氨基苯甲醛为底物传递 2-甲基喹唑啉3pa的概念验证； (iv)化合物3ga 、 3ja和3ma的克级合成。基于控制研究和氧化还原电位值，提出了还原猝灭机制。