2-(2-hydroxyphenyl)ethylamine hydrobromide | 13062-80-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-(2-hydroxyphenyl)ethylamine hydrobromide
• 英文别名: 2-hydroxyphenethylamine hydrobromide；2-(2-aminoethyl)phenol;hydrobromide
• CAS: 13062-80-1
• 化学式: BrH*C₈H₁₁NO
• 分子量: 218.093
• InChiKey: UIXYUFDRFYUTDF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.47
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  46.2
• 氢给体数：
  3
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-(2-hydroxyphenyl)ethylamine hydrobromide 在 盐酸 、 sodium nitrate 、 lanthanum(III) nitrate 作用下， 以 乙醚 为溶剂， 反应 25.0h， 生成 2-(2-hydroxy-3-nitrophenyl)-N-(trifluoroacetyl)ethylamine
  参考文献：
  名称：

  Synthesis and evaluation of non-catechol D-1 and D-2 dopamine receptor agonists: benzimidazol-2-one, benzoxazol-2-one, and the highly potent: benzothiazol-2-one 7-ethylamines

  摘要：

  Our interest in identifying D-1 and D-2 dopamine receptor agonists that are not catechols led us to extend previous studies with oxindoles by investigating analogues of dopamine, N,N-dipropyldopamine, m-tyramine, N,N-dipropyl-m-tyramine, and epinine in which the m-hydroxyl is replaced by the NH portion of a thiazol-2-one, oxazol-2-one, or imidazol-2-one group fused to the 2,3-position. These compounds were evaluated for their affinity and agonist activity at D-1 and D-2 receptors by using in vitro assays. Replacement of the m-hydroxy in N,N-dipropyldopamine with the thiazol-2-one group resulted in a dramatic increase in D-2 receptor affinity and activity compared to that of N,N-dipropyldopamine itself or that of the corresponding oxindole, 1. The resulting compound, 7-hydroxy-4-[2-(di-n-propylamino)ethyl]benzothiazol-2(3H)-one (4), is the most potent D-2 receptor agonist reported to date in the field-stimulated rabbit ear artery (ED50 = 0.028 nM). The benzoxazol-2-one (6), benzimidazol-2-one (5), and isatin (51) analogues showed D-2 receptor agonist potency similar to that of 1. The des-7-hydroxyl analogue of 4 (21) also has enhanced D-2 receptor activity compared to that of the corresponding oxindole, 8. 7-Hydroxy-4-(2-aminoethyl)benzothiazol-2(3H)-one, 27, a non-catechol, has enhanced D-1 and D-2 receptor activity in vitro compared to that of the corresponding oxindole, 7. In vivo, 27 increased renal blood flow and decreased blood pressure in the dog. However, these effects were mediated primarily by D-2 receptor agonist activity. This may be a result of the D-1 partial agonist activity of 27 coupled with its potent D-2 receptor activity.

  DOI：

  10.1021/jm00390a009

文献信息

• Compositions and methods for treating nephritis and inhibiting TGF -&bgr; related conditions using pyridylacrylamide derivatives
  申请人：Tsumura & Co.

  公开号：US06313153B1

  公开（公告）日：2001-11-06

  The present invention relates to an agent for treating nephritis and a TGF-&bgr; inhibiting agent comprising as an effective ingredient a pyridylacrylamide derivative represented by the following formula (I): wherein Ar1 is a substituted or unsubstituted pyridyl group, Ar2 is a substituted or unsubstituted phenyl group, R1 is a hydrogen atom, an alkyl group or an aryl group, R2 is a hydrogen atom, an alkyl group, a cyano group or an alkoxycarbonyl group, R3 is a hydrogen atom or an optionally substituted alkyl group, X is an oxygen or sulfur atom, A and B are same or different and each represent a hydrogen atom, a hydroxyl group, an alkoxy group or an alkylthio group, or A and B together form an oxo or thioxo group, or a group represented by the formula: ═N—Y in which Y is a dialkylamino, hydroxyl, aralkyloxy or alkoxy group, or a group represented by the formula: —Z1—M—Z2— which Z1 and Z2 are same or different and each represent an oxygen or sulfur atom or an imino group optionally substituted by an alkyl group, and M is an alkylene group or a 1,2-phenylene group, or A is a hydroxyl group and B is a 1-alkylimidazol-2-yl group, and n is an integer of 1 to 3, or a pharmaceutically acceptable salt thereof; as well as the pyridylacrylamide derivatives.

  本发明涉及一种用于治疗肾炎的药剂和一种TGF-β抑制剂，其有效成分为以下式(I)所表示的吡啶丙烯酰胺衍生物，其中Ar1是取代或未取代的吡啶基团，Ar2是取代或未取代的苯基团，R1是氢原子、烷基或芳基，R2是氢原子、烷基、氰基或烷氧羰基，R3是氢原子或可选择取代的烷基，X是氧原子或硫原子，A和B相同或不同，每个代表氢原子、羟基、烷氧基或烷基硫基，或A和B一起形成氧代或硫代基，或由式表示的基团：═N—Y，其中Y是二烷基氨基、羟基、芳基氧基或烷氧基，或由式表示的基团：—Z1—M—Z2—，其中Z1和Z2相同或不同，每个代表氧原子或硫原子或可选择由烷基取代的亚胺基，M是烷基或1,2-苯基，或A是羟基且B是1-烷基咪唑-2-基，n为1至3的整数，或其药学上可接受的盐；以及吡啶丙烯酰胺衍生物。
• 新規ピリミジン誘導体及びこれらを含有する抗菌剤
  申请人：Ｍｅｉｊｉ Ｓｅｉｋａファルマ株式会社

  公开号：JP2018154587A

  公开（公告）日：2018-10-04

  【課題】より効果の高いジヒドロ葉酸還元酵素阻害活性を有し、耐性菌を起因菌とする感染症に対する薬物治療の選択肢の幅を広げることができる新規化合物、またはその塩、及び前記新規化合物、またはその塩を含有する抗菌剤を提供すること、より効果の高いジヒドロ葉酸還元酵素阻害剤を提供することにある。【解決手段】下記式（Ｉ）で表される、２、４−ジアミノピリミジン骨格を有する化合物、またはその塩、前記化合物、またはその塩を有効成分とする抗菌剤を提供する。 【化１】【選択図】なし

  这个句子的翻译为：具有比叶酸还原酶抑制活性更高的新化合物，或其盐，可以扩大对抗耐药菌引起的感染症的药物治疗选择范围，同时提供包含该新化合物或其盐的抗菌剂，提供更有效的叶酸还原酶抑制剂。【解决方案】提供具有下述式（I）所示的2,4-二氨基嘌呤骨架的化合物，或其盐，以及以该化合物或其盐为有效成分的抗菌剂。【化1】【无图】
• Bezothiazol Derivatives as Beta2 Adrenoreceptor Agonists
  申请人：Alcaraz Lilian

  公开号：US20090062259A1

  公开（公告）日：2009-03-05

  The present invention relates to compounds according to formula (I), a process for preparing them, the intermediate compounds of the process and the use of the compounds in the manufacture of a medicament for use in treating diseases such as ARDS, pulmonary emphysema, bronchitis, bronchiectasis, COPD, asthma and rhinitis. The compounds are beta adrenoreceptor agonists.

  本发明涉及式(I)的化合物，其制备方法，该方法的中间体化合物以及化合物在制造治疗ARDS、肺气肿、支气管炎、支气管扩张、COPD、哮喘和鼻炎等疾病的药物中的应用。这些化合物是β-肾上腺素受体激动剂。
• Bezothiazol derivatives as Beta2 adrenoreceptor agonists
  申请人：AstraZeneca AB

  公开号：US07951954B2

  公开（公告）日：2011-05-31

  The present invention relates to compounds according to formula (I), a process for preparing them, the intermediate compounds of the process and the use of the compounds in the manufacture of a medicament for use in treating diseases such as ARDS, pulmonary emphysema, bronchitis, bronchiectasis, COPD, asthma and rhinitis. The compounds are beta adrenoreceptor agonists.

  本发明涉及公式（I）的化合物，其制备方法，该过程的中间体以及化合物在制造用于治疗ARDS，肺气肿，支气管炎，支气管扩张，COPD，哮喘和鼻炎等疾病的药物中的应用。这些化合物是β肾上腺素受体激动剂。
• PYRIDYLACRYLAMIDE DERIVATIVES AND NEPHRITIS REMEDIES AND TGF-$g(b) INHIBITORS CONTAINING THE SAME
  申请人：TSUMURA & CO.

  公开号：EP1000935A1

  公开（公告）日：2000-05-17

  The present invention relates to an agent for treating nephritis and a TGF-β inhibiting agent comprising as an effective ingredient a pyridylacrylamide derivative represented by the following formula (I): wherein Ar1 is a substituted or unsubstituted pyridyl group, Ar2 is a substituted or unsubstituted phenyl group, R1 is a hydrogen atom, an alkyl group or an aryl group, R2 is a hydrogen atom, an alkyl group, a cyano group or an alkoxycarbonyl group, R3 is a hydrogen atom or an optionally substituted alkyl group, X is an oxygen or sulfur atom. A and B are same or different and each represent a hydrogen atom, a hydroxyl group, an alkoxy group or an alkylthio group, or A and B together form an oxo or thioxo group, or a group represented by the formula: =N-Y in which Y is a dialkylamino, hydroxyl, aralkyloxy or alkoxy group, or a group represented by the formula: -Z1-M-Z2- in which Z1 and Z2 are same or different and each represent an oxygen or sulfur atom or an imino group optionally substituted by an alkyl group, and M is an alkylene group or a 1,2-phenylene group, or A is a hydroxyl group and B is a 1-alkylimidazol-2-yl group, and n is an integer of 1 to 3, or a pharmaceutically acceptable salt thereof; as well as the pyridylacrylamide derivatives.

  本发明涉及一种治疗肾炎的制剂和一种 TGF-β 抑制剂，其有效成分包括下式 (I) 所代表的吡啶丙烯酰胺衍生物： 其中 Ar1 是取代或未取代的吡啶基，Ar2 是取代或未取代的苯基，R1 是氢原子、烷基或芳基，R2 是氢原子、烷基、氰基或烷氧羰基，R3 是氢原子或任选取代的烷基，X 是氧原子或硫原子。A 和 B 相同或不同，各自代表一个氢原子、一个羟基、一个烷氧基或一个烷硫基，或 A 和 B 共同形成一个氧代或硫代基团，或一个由式：=N-Y 所代表的基团，其中 Y 是一个二烷基氨基、羟基、芳氧基或烷氧基，或一个由式： -Z1-M-Z2- 所代表的基团，其中 Y 是一个二烷基氨基、羟基、芳氧基或烷氧基：-Z1-M-Z2-，其中 Z1 和 Z2 相同或不同，且各自代表氧原子或硫原子或任选被烷基取代的亚氨基，M 为亚烷基或 1,2-亚苯基，或 A 为羟基，B 为 1-烷基咪唑-2-基，n 为 1 至 3 的整数、 或其药学上可接受的盐；以及吡啶丙烯酰胺衍生物。