2-氨基-3,4-二氢-1(2H)-萘酮 | 60505-03-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 中文名称: 2-氨基-3,4-二氢-1(2H)-萘酮
• 英文名称: 2-amino-1,2,3,4-tetrahydronaphthalen-1-one
• 英文别名: 2-amino-3,4-dihydronaphthalen-1(2H)-one；2-amino-3,4-dihydro-2H-naphthalen-1-one；(+/-)-2-Amino-1-oxo-1.2.3.4-tetrahydro-naphthalin；2-Amino-3,4-dihydro-2H-naphthalin-1-on；2-amino-1-tetralone；2-Amino-1-keto-1.2.3.4-tetrahydronaphthalene；2-Amino-3,4-dihydro-2H-naphthalen-1-one
• CAS: 60505-03-5
• 化学式: C₁₀H₁₁NO
• mdl: MFCD09036215
• 分子量: 161.203
• InChiKey: MUGWUYGVUZLWRB-UHFFFAOYSA-N

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：
  0.3
• 拓扑面积：
  43.1
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-氨基-3,4-二氢-1(2H)-萘酮 在 lithium aluminium tetrahydride 作用下， 以 乙醚 为溶剂， 生成 trans-2-amino-1,2,3,4-tetrahydro-1-naphthalenol
  参考文献：
  名称：

  Lukes,R. et al., Collection of Czechoslovak Chemical Communications, 1960, vol. 25, p. 492 - 501

  摘要：

  DOI：
• 作为产物：
  描述：

  2-hydroxyimino-3,4-dihydro-2H-1-naphthalenone 在 palladium on barium sulfate 盐酸 、 氢气 作用下， 以 甲醇 为溶剂， 生成 2-氨基-3,4-二氢-1(2H)-萘酮
  参考文献：
  名称：

  Aminotetralins as narcotic antagonists. Synthesis and opiate-related activity of 1-phenyl-1-aminotetralin derivatives

  摘要：

  The synthesis and the opiate agonist and antagonist activities of three derivatives of cis-2-[methyl(cyclopropanemethyl)amino]-1-phenyltetralin are reported. The compounds were obtained by synthetic modification from 2-amino-1-tetralone. The 1-propionoxy derivative 4c shows analgetic activity (ED50 = 17.8 mg/kg) one-half that of codeine, and the 1-methoxy derivative 4b has weak antagonist activity (AD50 = 33.5 mg/kg). The compounds showed no other significant opiate-related activity.

  DOI：

  10.1021/jm00188a017

文献信息

• Flexible Stereoselective Functionalizations of Ketones through Umpolung with Hypervalent Iodine Reagents
  作者：Pushpak Mizar、Thomas Wirth

  DOI：10.1002/anie.201400405

  日期：2014.6.2

  The functionalization of carbonyl compounds in the α‐position has gathered much attention as a synthetic route because of the wide biological importance of such products. Through polarity reversal, or “umpolung”, we show here that typical nucleophiles, such as oxygen, nitrogen, and even carbon nucleophiles, can be used for addition reactions after tethering them to enol ethers. Our findings allow novel

  由于此类产品具有广泛的生物学重要性，因此羰基化合物在α位上的功能化作为合成途径已引起广泛关注。通过极性反转或“极性”，我们在这里表明典型的亲核试剂，例如氧，氮，甚至碳亲核试剂，在将它们束缚到烯醇醚后，可以用于加成反应。我们的发现可以进行新颖的逆合成规划，并可以快速组装以前只能通过多步序列访问的结构。
• Rigidized oxazole dyes
  申请人：The United States of America as represented by the Secretary of the Navy

  公开号：USH0000753H1

  公开（公告）日：1990-03-06

  The quaternary salts of rigidized 1,3-oxazole compounds of the formula: ##STR1## where R is either H or CH.sub.3 O. The compounds are produced in a modif Robinson-Gabriel synthesis of oxazoles. These dyes are used in solution with non-interfering polar solvents, such as ethanol and H.sub.2 O, to form lasing media useful in dye lasers.

  刚性化的1,3-噁唑化合物的第四級盐的公式为：##STR1##其中R是H或CH.sub.3 O。这些化合物是通过改进的Robinson-Gabriel噁唑合成法生产的。这些染料与不干扰极性溶剂（例如乙醇和H.sub.2 O）一起使用，形成用于染料激光器的激光介质。
• 2-(CYCLIC AMINO)-PYRIMIDONE DERIVATIVES
  申请人：Fukunaga Kenji

  公开号：US20090233918A1

  公开（公告）日：2009-09-17

  A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R 2 represents a hydrogen or the like; R 3 represents methyl group or the like; R 20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R 4 represents hydrogen or the like; R 5 represents hydrogen or the like; R 6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH 2 , oxygen atom, NH, or the like; any one or more of R 5 and R 6 , R 5 and R 4 , R 6 and R 4 , X and R 5 , X and R 4 , X and R 6 , and R 6 and R 6 may combine to each other to form a ring, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).

  化合物的化学式为（I），其手性异构体或药物可接受的盐：其中，R2代表氢或类似物；R3代表甲基基团或类似物；R20代表卤素原子或类似物；q表示0到3的整数；Z代表氮原子，CH或类似物；R4代表氢或类似物；R5代表氢或类似物；R6代表取代的烷氧基或类似物；p表示0到3的整数；X代表键，CH2，氧原子，NH或类似物；R5和R6，R5和R4，R6和R4，X和R5，X和R4，X和R6以及R6和R6中的任何一个或多个可以结合形成环，用于预防和/或治疗由tau蛋白激酶1过度活化引起的疾病，例如神经退行性疾病（例如阿尔茨海默病）。
• Hexahydronaphth(1,2-b)-1,4-oxazines, process for their preparation and pharmaceutical formulation containing them
  申请人：Merck & Co., Inc.

  公开号：EP0080115A2

  公开（公告）日：1983-06-01

  Hexahydronaphth[1,2-b]-1,4-oxazines have dopaminergic activity and display α2-adrenergic receptor antagonism. They are useful in the treatment of parkinsonism, depression and hypertension. An important method of preparation is by ring closure of the appropriate 2-chloroacetamido- tetrahydronaphthalen-1-ol and reduction of the resulting cyclic amide carbonyl group.

  六氢萘并[1,2-b]-1,4-噁嗪具有多巴胺能活性，并显示出α2-肾上腺素能受体拮抗作用。 它们可用于治疗帕金森病、抑郁症和高血压。 一种重要的制备方法是将适当的 2-氯乙酰胺基四氢萘-1-醇闭环，并还原由此产生的环状酰胺羰基。
• Neber; Burgard; Thier, Justus Liebigs Annalen der Chemie, 1936, vol. 526, p. 277,287
  作者：Neber、Burgard、Thier

  DOI：——

  日期：——