7-氨基-2-萘酚盐酸盐 | 51761-16-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 中文名称: 7-氨基-2-萘酚盐酸盐
• 英文名称: 7-aminonaphthol hydrochloride
• 英文别名: 7-hydroxy-2-naphthylamine hydrochloride；7-amino-2-naphthol hydrochloride；7-aminonaphthalen-2-ol;hydrochloride
• CAS: 51761-16-1
• 化学式: C₁₀H₉NO*ClH
• 分子量: 195.648
• InChiKey: VDFLTUHMDULKQC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.55
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  46.2
• 氢给体数：
  3
• 氢受体数：
  2

安全信息

• 海关编码：
  2922299090
• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335

反应信息

• 作为反应物：
  描述：

  7-氨基-2-萘酚盐酸盐 在 sodium methylate 、 三乙胺 作用下， 以 四氢呋喃 为溶剂， 反应 25.0h， 生成 N-[7-(quinolin-2-ylmethoxy)naphthalen-2-yl]methanesulfonamide
  参考文献：
  名称：

  N-[(Arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene d4 antagonists of novel structure

  摘要：

  Two series of compounds, N-[(arylmethoxy)phenyl] sulfonamides and N-[(arylmethoxy)naphthyl] sulfonamides, were prepared as leukotriene D4 (LTD4) antagonists. In the phenyl series, N-[3-(2-quinolinylmethoxy)phenyl]-trifluoromethanesulfonamide (Wy-48,252, 16) was the most potent inhibitor of LTD4-induced bronchoconstriction in the guinea pig. With an intragastric ID50 of 0.1 mg/kg (2-h pretreatment), 16 was 300 times more potent than LY-171,883. Compound 16 also intragastrically inhibited ovalbumin-induced bronchoconstriction in the guinea pig with an ID50 of 0.6 mg/kg. In vitro against LTD4-induced contraction of isolated guinea pig trachea pretreated with indomethacin and L-cysteine, 16 produced a pKB value of 7.7. In the rat PMN assay 16 inhibited both 5-lipoxygenase and cyclooxygenase (IC50's = 4.6 and 3.3 microM). In the naphthyl series, N-[7-(2-quinolinylmethoxy)-2-naphthyl]trifluoromethanesulfonamide (Wy-48,090, 47) in addition to potent LTD4 antagonist activity (on isolated guinea pig trachea 47 had a pKB value of 7.04) also had antiinflammatory activity (63% inhibition at 50 mg/kg in the rat carrageenan paw edema assay and 34% inhibition of TPA-induced inflammation at 1 mg/ear in the mouse ear edema model). Perhaps the antiinflammatory activity of 47 was due to its additional activity of inhibiting both 5-lipoxygenase and cyclooxygenase enzymes (IC50's = 0.23 and 11.9 microM, respectively, in rat PMN).

  DOI：

  10.1021/jm00126a006

文献信息

• Quinolinyl (or pyridinyl) methoxy substituted naphthalene compounds as
  申请人：American Home Products Corporation

  公开号：US04661596A1

  公开（公告）日：1987-04-28

  There are disclosed compounds of the formula ##STR1## wherein X is --Ch.sub.2 CH.sub.2 --, --CH=CH--, ##STR2## Z is CR or N, when n=1; or Z is O, S, or NR, when n=0; R is hydrogen or loweralkyl; n is 0 or 1; R.sup.1 is hydroxy, amino, loweralkyl sulfonamido, perfluoro loweralkyl sulfonamido or OR; R.sup.2 is hydrogen or loweralkyl; R.sup.3 is hydrogen or loweralkyl; or R.sup.2 and R.sup.3 taken together form a benzene ring; and the dotted line represents an optional double bond; and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like.

  已披露的化合物的结构式为##STR1##其中X为--Ch.sub.2 CH.sub.2 --，--CH=CH--，##STR2##Z为CR或N，当n=1时；或Z为O，S或NR，当n=0时；R为氢或低碳烷基；n为0或1；R.sup.1为羟基，氨基，低碳烷基磺酰胺基，全氟低碳烷基磺酰胺基或OR；R.sup.2为氢或低碳烷基；R.sup.3为氢或低碳烷基；或R.sup.2和R.sup.3一起形成苯环；虚线表示可选的双键；及其药用盐，以及它们在治疗白三烯介导的鼻支气管阻塞气道疾病，如过敏性鼻炎，过敏性支气管哮喘等方面的用途。
• Herbicidal (hetero)aryloxynaphthalene derivatives and intermediates
  申请人：Bayer Aktiengesellschaft

  公开号：US05068394A1

  公开（公告）日：1991-11-26

  Herbicidal (hetero)aryloxynaphthalene derivatives of the formula ##STR1## in which X is N or --C--R.sup.5, R.sup.1, R.sup.2, R.sup.4 and R.sup.5 are hydrogen or halogen or R.sup.1 may be cyano or trifluoromethyl, R.sup.3 is halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio or trifluoromethylsulphonyl, Y is optionally halogen-substituted alkanediyl or alkenediyl, and Z is CN or --CC--Z', where Z' is halogen, hydroxyl, amine, alkoxy, or the like. Intermediates of the formula ##STR2## are also new.

  式子为 ##STR1## 的除草剂（杂）芳氧基萘衍生物，其中 X 为 N 或 --C--R.sup.5，R.sup.1、R.sup.2、R.sup.4 和 R.sup.5 为氢或卤素，或者 R.sup.1 可为氰基或三氟甲基，R.sup.3 为卤素、三氟甲基、三氟甲氧基、三氟甲硫基或三氟甲基磺酰基，Y 为可选卤素取代的烷二基或烯二基，Z 为 CN 或 --CC--Z'，其中 Z' 为卤素、羟基、胺、烷氧基或类似物。式子为 ##STR2## 的中间体也是新的。
• Imidazolylmethoxy naphthalene compounds as antiallergic agents
  申请人：American Home Products Corporation

  公开号：US04719308A1

  公开（公告）日：1988-01-12

  There are disclosed compounds of the formula ##STR1## wherein X is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## Z is CR or N, when n=1; or Z is O, S, or NR, when n=0, R is hydrogen or loweralkyl; n is 0 or 1; R.sup.1 is hydroxy, amino, loweralkyl sulfonamido, perfluoro loweralkyl sulfonamido or OR; R.sup.2 is hydrogen or loweralkyl; R.sup.3 is hydrogen or loweralkyl; or R.sup.2 and R.sup.3 taken together form a benzene ring; and the dotted line represents an optional double bond; and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like.

  公开了如下式的化合物：##STR1## 其中X为--CH.sub.2 CH.sub.2 --，--CH.dbd.CH--，##STR2## 当n=1时，Z为CR或N；或当n=0时，Z为O、S或NR，R为氢或低碳基；n为0或1；R.sup.1为羟基、氨基、低碳基磺酰胺基、全氟低碳基磺酰胺基或OR；R.sup.2为氢或低碳基；R.sup.3为氢或低碳基；或R.sup.2和R.sup.3共同形成苯环；虚线代表可选的双键；以及其药学上可接受的盐，并用于治疗白三烯介导的鼻支气管阻塞性通气道疾病，例如过敏性鼻炎、过敏性支气管哮喘等。
• Oxazole and thiazole naphthalenes as antiallergic agents
  申请人：American Home Products Corporation

  公开号：US04754043A1

  公开（公告）日：1988-06-28

  There are disclosed compounds of the formula ##STR1## wherein X is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## Z is CR or N, where n=1; or Z is O,S, or NR, when n=0; R is hydrogen or loweralkyl; n is 0 or 1; R.sup.1 is hydroxy, amino, loweralkyl sulfonamido, perfluoro loweralkyl sulfonamido or OR; R.sup.2 is hydrogen or loweralkyl; R.sup.3 is hydrogen or loweralkyl; or R.sup.2 and R.sup.3 taken together form a benzene ring; and the dotted line represents an optional double bond; and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like.

  公开了化合物的结构式，其中X为--CH.sub.2 CH.sub.2 --，--CH.dbd.CH--，##STR2##Z为CR或N，其中n=1; 或者Z为O，S或NR，当n=0时; R为氢或低碳基; n为0或1; R.sup.1为羟基，氨基，低碳基磺酰胺基，全氟低碳基磺酰胺基或OR; R.sup.2为氢或低碳基; R.sup.3为氢或低碳基; 或者R.sup.2和R.sup.3结合形成苯环; 虚线代表可选的双键;及其药学上可接受的盐，以及它们在治疗白三烯介导的鼻-支气管阻塞性通气道疾病，如过敏性鼻炎，过敏性支气管哮喘等方面的用途。
• John; Weber, Journal fur praktische Chemie (Leipzig 1954), 1925, vol. <2>111, p. 87
  作者：John、Weber

  DOI：——

  日期：——