5-amino-1-hydroxy-5,6,7,8-tetrahydronaphthalene | 90874-84-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: 5-amino-1-hydroxy-5,6,7,8-tetrahydronaphthalene
• 英文别名: 5-hydroxy-1-aminotetralin；5-Amino-5,6,7,8-tetrahydro-[1]naphthol；1-Amino-5-oxy-naphthalin-tetrahydrid-(1.2.3.4)；5-Amino-5,6,7,8-tetrahydronaphthalen-1-ol
• CAS: 90874-84-3
• 化学式: C₁₀H₁₃NO
• 分子量: 163.219
• InChiKey: JGBIMURCUPHILK-UHFFFAOYSA-N

物化性质

• 熔点：
  209-210 °C
• 沸点：
  295.5±40.0 °C(Predicted)
• 密度：
  1.147±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  46.2
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  5-amino-1-hydroxy-5,6,7,8-tetrahydronaphthalene 在 2-二甲氨基吡啶 、 氢氧化钾 、 乙酸酐 、 三乙胺 作用下， 以 甲醇 、 乙酸乙酯 为溶剂， 生成 N-(5-hydroxy-1,2,3,4-tetrahydro-[1]naphthyl)-acetamide
  参考文献：
  名称：

  Substituted amino-5,6,7,8-tetrahydronaphthyl-oxyacetic acids, processes

  摘要：

  公式为##STR1##的抗血栓、抗动脉粥样硬化和抗缺血化合物，其中R.sup.1是##STR2##或SO.sub.2R.sup.4，R.sup.3是芳基、取代芳基、杂环芳基、芳基烷基或基团##STR3##，R.sup.4是芳基或取代芳基，R.sup.2是OH、烷氧基、苯氧基、苯甲氧基或NR.sup.5R.sup.6，R.sup.5和R.sup.6各自独立地是氢或烷基，或者其中的一个基团R.sup.5或R.sup.6是苄基，以及其与一价和二价阳离子形成的生理上可接受的盐。

  公开号：

  US04868331A1
• 作为产物：
  描述：

  alkaline earth salt of/the/ methylsulfuric acid 在 盐酸 、 水 、 sodium nitrite 作用下， 生成 5-amino-1-hydroxy-5,6,7,8-tetrahydronaphthalene
  参考文献：
  名称：

  Bamberger; Bammann, Chemische Berichte, 1889, vol. 22, p. 964

  摘要：

  DOI：

文献信息

• [EN] NOVEL PHENYL IMIDAZOLES AND PHENYL TRIAZOLES AS GAMMA-SECRETASE MODULATORS<br/>[FR] NOUVEAUX PHÉNYL IMIDAZOLES ET PHÉNYL TRIAZOLES EN TANT QUE MODULATEURS DE LA GAMMA SÉCRÉTASE
  申请人：PFIZER

  公开号：WO2010100606A1

  公开（公告）日：2010-09-10

  Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

  所述化合物及其药用可接受盐已被披露，其中所述化合物具有规范中定义的Formula (I)的结构。相应的药物组合物、治疗方法、合成方法和中间体也已被披露。
• N6-SUBSTITUTED ADENOSINE DERIVATIVES AND N6-SUBSTITUTED ADENINE DERIVATIVES AND USES THEREOF
  申请人：Shi Jiangong

  公开号：US20130045942A1

  公开（公告）日：2013-02-21

  The present invention provides N 6 -substituted adenosine derivatives and N 6 -substituted adenine derivatives, manufacturing methods thereof, a pharmaceutical composition comprising the said compounds above, and uses of these compounds in manufacturing medicaments and health-care products for treating insomnia, convulsion, epilepsy, and Parkinson's diseases, and preventing and treating dementia.

  本发明提供了N6-取代腺苷衍生物和N6-取代腺嘌呤衍生物，其制备方法，包括上述化合物的药物组合物，以及这些化合物在制造治疗失眠、惊厥、癫痫和帕金森病的药物和保健产品以及预防和治疗痴呆症中的用途。
• Novel Phenyl Imidazoles and Phenyl Triazoles As Gamma-Secretase Modulators
  申请人：Allen Martin Patrick

  公开号：US20120053165A1

  公开（公告）日：2012-03-01

  Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

  本发明公开了具有式（I）所定义的结构的化合物及其药学上可接受的盐，同时公开了相应的制药组合物、治疗方法、合成方法和中间体。
• N6-substituted adenosines
  申请人：WARNER-LAMBERT COMPANY

  公开号：EP0179667A2

  公开（公告）日：1986-04-30

  There is disclosed a compound of the following general formula (I): its diastereomer, or a pharmaceutically acceptable acid addition salt thereof; wherein R1 is of the formula or in which; n is an integer of from one to four; Z is hydrogen, lower alkyl or hydroxy; Y is hydrogen, lower alkyl, or OR where R is hydrogen, lower alkyl or lower alkanoyl; A is a bond or a straight or branched alkylene of from one to four carbon atoms, with the proviso that A cannot be a bond when R1 is of Formula II and n is one; X and X' are each, independently, hydrogen, lower alkyl, lower alkoxy, hydroxy, lower alkanoyl, nitro, trifluoromethyl, halogen, amino, monolower-alkyl or diloweralkylamino, or when taken X and X' together are a methylenedioxy group; R2 is a) hydrogen, b) halogen, c) NR'R" where R' and R" are independently hydrogen, lower alkyl, phenyl, or phenyl substituted by lower alkyl, lower alkoxy, halogen, or trifluoromethyl, d) SR'" where R" is hydrogen, lower alkyl, lower alkanoyl, benzoyl, or phenyl; R'2, R'3 and R'e are each, independently, hydrogen, alkanoyl having two to twelve carbon atoms, inclusive, in a straight or branched alkyl chain, benzoyl, or benzoyl substituted by lower alkyl, lower alkoxy, halogen, or R'2 and R'3 taken together are a five- membered ring having a total of up to twenty carbons; or R'e is, independently, a phosphate, hydrogen, or dihydrogen phosphate, or an alkali metal or ammonium, or dialkali or diammonium salt thereof; with the proviso that overall when R1 is II and X' X', Y, and Z are hydrogen, or lower alkyl then n cannot be two. The novel N6-substituted adenosines have desirable ratio of affinities at A1 or A2 receptors and highly desirable central nervous system and cardiovascular activities, such as analgesic, antipsychotic, sedative, or antihypertensive as well as immunoinflammatory activity.

  本发明公开了一种通式（I）如下的化合物： 其非对映异构体，或其药学上可接受的酸 加成盐； 其中 R1 为式 或 其中 n 是 1 到 4 的整数； Z 是氢、低级烷基或羟基； Y 是氢、低级烷基或 OR，其中 R 是氢、低级烷基或低级烷酰基； A 是键或 1 至 4 个碳原子的直链或支链亚烷基，但当 R1 为式 II 且 n 为 1 时，A 不能为键； X和X'各自独立地为氢、低级烷基、低级烷氧基、羟基、低级烷酰基、硝基、三氟甲基、卤素、氨基、单低级烷基或稀低烷基氨基，或当X和X'合在一起时为亚甲基二氧基； R2 是 a) 氢，b) 卤素，c) NR'R"，其中 R' 和 R "独立地是氢、低级烷基、苯基或被低级烷基、低级烷氧基、卤素或三氟甲基取代的苯基，d) SR'"，其中 R" 是氢、低级烷基、低级烷酰基、苯甲酰基或苯基； R'2、R'3 和 R'e 各自独立地是氢、在直链或支链烷基中具有 2 至 12 个碳原子的烷酰基、苯甲酰基或被低级烷基、低级烷氧基、卤素取代的苯甲酰基，或 R'2 和 R'3 合在一起是一个总碳数不超过 20 个的五元环；或 R'e 独立地是磷酸、氢或磷酸二氢、或碱金属或铵、或二碱或二铵盐；但总体上，当 R1 是 II 且 X' X'、Y 和 Z 是氢、或低级烷基时，则 n 不能为 2。 新型 N6 取代腺苷在 A1 或 A2 受体上具有理想的亲和力比率，并具有非常理想的中枢神经系统和心血管活性，如镇痛、抗精神病、镇静或抗高血压以及免疫炎症活性。
• N6-SUBSTITUTED ADENOSINE DERIVATIVES, N6-SUBSTITUTED ADENINE DERIVATIVES AND USES THEREOF
  申请人：INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF MEDICAL SCIENCES

  公开号：EP2511283A1

  公开（公告）日：2012-10-17

  The present invention provides N6-substituted adenosine derivatives and N6-substituted adenine derivatives, manufacturing methods thereof, a pharmaceutical composition comprising the said compounds above, and uses of of these compounds in manufacturing medicaments and health-care products for treating insomnia, convulsion, epilepsy, and Parkinson's diseases, and preventing and treating dementia.

  本发明提供了 N6-取代腺苷衍生物和 N6-取代腺嘌呤衍生物、其制造方法、包含上述化合物的药物组合物，以及这些化合物在制造治疗失眠、抽搐、癫痫和帕金森病以及预防和治疗痴呆症的药物和保健产品中的用途。