2-chloro-N-(2-hydroxy-4-methoxyphenyl)acetamide | 6529-91-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 酚类
• 英文名称: 2-chloro-N-(2-hydroxy-4-methoxyphenyl)acetamide
• 英文别名: 2-Chloroacetamido-5-methoxy phenol
• CAS: 6529-91-5
• 化学式: C₉H₁₀ClNO₃
• 分子量: 215.636
• InChiKey: KLTKUGKSHUTBFE-UHFFFAOYSA-N

物化性质

• 熔点：
  158-160 °C(Solv: ethanol (64-17-5))
• 沸点：
  424.0±45.0 °C(Predicted)
• 密度：
  1.379±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  58.6
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-chloro-N-(2-hydroxy-4-methoxyphenyl)acetamide 在 sodium iodide potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 7-甲氧基-2H-苯并[b][1,4]噁嗪-3(4H)-酮
  参考文献：
  名称：

  Production Method of Nitrogen-Containing Fused Ring Compounds

  摘要：

  本发明提供了一种优越的化合物生产方法和优越的纯化方法，用于治疗或预防涉及尿酸的病理学，如高尿酸血症、痛风石、急性痛风性关节炎、慢性痛风性关节炎、痛风性肾脏、尿路结石、肾功能障碍、冠状动脉疾病、缺血性心脏病等。 [手段] 通过将以下式[3]所代表的化合物或其盐与以下式[4]所代表的化合物、其盐或其反应衍生物反应，可以制备以下式[2]所代表的化合物或其药用可接受的盐。此外，可以以工业上优越的可操作性进行以下式[2]所代表的化合物的结晶，并且可以获得以下式[2]所代表的化合物的高质量晶体。 其中每个符号如描述中所定义。

  公开号：

  US20080064871A1
• 作为产物：
  描述：

  2,4-二甲氧基苯胺 在 三氯化铝 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 17.0h， 生成 2-chloro-N-(2-hydroxy-4-methoxyphenyl)acetamide
  参考文献：
  名称：

  Synthesis of D-oxa tricyclic partial ergolines as dopamine agonists

  摘要：

  A series of hetero fused hexahydro-1,4-benzoxazines has been synthesized and evaluated for dopamine agonist activity. This class of compounds is another example in which an oxygen substitution in the D ring of a partial ergoline or ergoline retains dopaminergic properties. Compound 10, trans-(+/-)-4,4a,5,6,8a,9-hexahydro-5-propyl-2H,7H-pyrazolo[4,3-g] [1,4]benzoxazine, is a D-ring analogue of trans-(+/-)-4,4a,5,6,7,8,8a,9-octahydro-5-propyl-2H-pyrazolo[3,4-g]qu ino line (1, LY141865) and also a des-A-ring analogue of 9-oxaergoline. Compounds 10, 2-aminohexahydrothiazolo[1,4]benzoxazine 11, and 2-aminohexahydropyrimido[1,4]benzoxazine 12 possess dopaminergic activity in prolactin inhibition and 6-hydroxydopamine lesioned rat turning assays.

  DOI：

  10.1021/jm00386a023

文献信息

• Npy antagonists, preparation and uses
  申请人：Botez Iuliana

  公开号：US20090233910A1

  公开（公告）日：2009-09-17

  The present invention concerns novel compounds, their preparation and their uses, therapeutic uses in particular. More specifically it concerns derivative compounds having at least two aromatic cycles, their preparation and their uses, in particular in the area of human or animal health. These compounds have an affinity for the biological receptors of neuropeptide Y, NPY, present in the central and peripheral nervous systems. The compounds of the invention are preferably NPY antagonists, and more particularly antagonists of sub-type NPY Y1, and can therefore be used for the therapeutic or prophylactic treatment of any disorder involving NPY. The present invention also concerns pharmaceutical compositions containing said compounds, their preparation and their uses, as well as treatment methods using said compounds.

  本发明涉及新颖化合物，它们的制备和用途，特别是在治疗方面的用途。更具体地说，它涉及至少具有两个芳香环的衍生化合物，它们的制备和用途，特别是在人类或动物健康领域。这些化合物对存在于中枢和外周神经系统中的神经肽Y（NPY）的生物受体具有亲和力。本发明的化合物优选为NPY拮抗剂，更具体地说是NPY Y1亚型的拮抗剂，因此可用于治疗或预防涉及NPY的任何疾病。本发明还涉及含有所述化合物的药物组合物，其制备和用途，以及使用所述化合物的治疗方法。
• Nitrogen-containing fused ring compounds and use thereof
  申请人：Hirata Kazuyuki

  公开号：US20070010670A1

  公开（公告）日：2007-01-11

  A URAT1 activity inhibitor containing a nitrogen-containing fused ring compound represented by the following formula [1]: wherein each symbol is as defined in the description. The present invention is useful for the prophylaxis or treatment of pathology showing involvement of uric acid, such as hyperuricemia, gouty tophus, acute gouty arthritis, chronic gouty arthritis, gouty kidney, urolithiasis, renal function disorder, coronary artery disease, ischemic heart disease and the like.

  一种包含氮含有融合环化合物的URAT1活性抑制剂，其化学式如下所示[1]： 其中每个符号如描述中所定义。本发明对于预防或治疗显示尿酸参与的病理学，如高尿酸血症、痛风石、急性痛风性关节炎、慢性痛风性关节炎、痛风性肾脏、尿路结石、肾功能障碍、冠状动脉疾病、缺血性心脏病等方面具有用处。
• Pharmaceutical Compositions Comprising Nitrogen-Containing Fused Ring Coumpounds
  申请人：Miki Kazuki

  公开号：US20080305169A1

  公开（公告）日：2008-12-11

  [Problems] The present invention provides pharmaceutical composition which is effective for the prophylaxis or treatment of pathology showing involvement of uric acid (hyperuricemia, gouty tophus, acute gout arthritis, chronic gout arthritis, gouty kidney, urolithiasis, renal function disorder, coronary arterial disease, ischemic heart disease and the like) and the like, and is superior in the time-course stability and dissolution property (disintegration property). [Solving Means] The pharmaceutical composition of the present invention is a pharmaceutical composition comprising a nitrogen-containing fused ring compound represented by the following formula [1] or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable additives, wherein the nitrogen-containing fused ring compound or a pharmaceutically acceptable salt thereof is not in contact with a basic additive: wherein each symbol is as described in the specification.

  本发明提供了一种药物组合物，用于预防或治疗涉及尿酸的病理（高尿酸血症、痛风石、急性痛风性关节炎、慢性痛风性关节炎、痛风性肾脏、尿路结石、肾功能障碍、冠状动脉疾病、缺血性心脏病等），并且在时间稳定性和溶解性（分解性）方面具有优越性。 【解决手段】本发明的药物组合物是一种药物组合物，包括下式【1】所表示的含氮融合环化合物或其药学上可接受的盐，以及一种或多种药学上可接受的添加剂，其中所述的含氮融合环化合物或其药学上可接受的盐与碱性添加剂不接触： 其中每个符号如说明书中所述。
• Production Method of Nitrogen-Containing Fused Ring Compounds
  申请人：Hirata Kazuyuki

  公开号：US20080064871A1

  公开（公告）日：2008-03-13

  [Problems] The present invention provides a superior production method and a superior purification method of compounds effective for the treatment or prophylaxis of pathology showing involvement of uric acid, such as hyperuricemia, gouty tophus, acute gouty arthritis, chronic gouty arthritis, gouty kidney, urolithiasis, renal function disorder, coronary artery disease, ischemic heart disease and the like. [Means] A compound represented by the following formula [2] or a pharmaceutically acceptable salt thereof can be produced by reacting a compound represented by the following formula [3] or a salt thereof with a compound represented by the following formula [4], a salt thereof or a reactive derivative thereof. Moreover, crystallization of a compound represented by the formula [2] can be performed with industrially superior workability, and high quality crystals of a compound represented by the formula [2] can be obtained. wherein each symbol is as defined in the description.

  本发明提供了一种优越的化合物生产方法和优越的纯化方法，用于治疗或预防涉及尿酸的病理学，如高尿酸血症、痛风石、急性痛风性关节炎、慢性痛风性关节炎、痛风性肾脏、尿路结石、肾功能障碍、冠状动脉疾病、缺血性心脏病等。 [手段] 通过将以下式[3]所代表的化合物或其盐与以下式[4]所代表的化合物、其盐或其反应衍生物反应，可以制备以下式[2]所代表的化合物或其药用可接受的盐。此外，可以以工业上优越的可操作性进行以下式[2]所代表的化合物的结晶，并且可以获得以下式[2]所代表的化合物的高质量晶体。 其中每个符号如描述中所定义。
• Diaminopyrimidines as P2X3 and P2X2/3 antagonists
  申请人：Broka Allen Chris

  公开号：US20050209260A1

  公开（公告）日：2005-09-22

  Compounds and methods for treating diseases mediated by a P2X 3 and/or a P2X 2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein D, X, Y, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined herein.

  用于治疗由P2X3和/或P2X2/3受体拮抗剂介导的疾病的治疗化合物和方法，该方法包括向有需要的受试者施用有效量的式I化合物：或其药学上可接受的盐、溶剂化物或前药，其中D、X、Y、R1、R2、R3、R4、R5、R6、R7和R8如本文所定义。