5-(aminomethyl)-5,6,7,8-tetrahydro-2-naphthalenamine | 1073633-40-5

• 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-(aminomethyl)-5,6,7,8-tetrahydro-2-naphthalenamine
• 英文别名: 5-Aminomethyl-5,6,7,8-tetrahydro-naphthalen-2-ylamine；5-(aminomethyl)-5,6,7,8-tetrahydronaphthalen-2-amine
• CAS: 1073633-40-5
• 化学式: C₁₁H₁₆N₂
• 分子量: 176.261
• InChiKey: MGLNDEAUQQIPOP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  52
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  5-(aminomethyl)-5,6,7,8-tetrahydro-2-naphthalenamine 在 palladium 10% on activated carbon 盐酸 、 manganese(IV) oxide 、 potassium tert-butylate 、 氢气 、 碳酸氢钠 、 potassium carbonate 、 三乙胺 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 甲醇 、 乙醇 、 二氯甲烷 、 氯仿 、 N,N-二甲基甲酰胺 、 乙腈 为溶剂， 反应 7.67h， 生成 4-(5-{[(6,7-dihydro[1,4]dioxino[2,3-c]pyridazin-3-ylmethyl)amino]-methyl}-5,6,7,8-tetrahydro-2-naphthalenyl)-6-(methyloxy)pyrido[2,3-b]pyrazin-3(4H)-one
  参考文献：
  名称：

  WO2008/128961

  摘要：

  公开号：
• 作为产物：
  描述：

  6-氨基-1,2,3,4-四氢-1-萘酮 在 镍 sodium tetrahydroborate 、 lithium methanolate 、 氨 、 氢气 、 对甲苯磺酸 作用下， 以 四氢呋喃 、 乙醇 、 水 、 甲苯 为溶剂， 20.0~40.0 ℃ 、350.01 kPa 条件下， 反应 2.0h， 生成 5-(aminomethyl)-5,6,7,8-tetrahydro-2-naphthalenamine
  参考文献：
  名称：

  WO2008/128961

  摘要：

  公开号：

文献信息

• [EN] AMINOMETHYL SUBSTITUTED BICYCLIC AROMATIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR<br/>[FR] COMPOSES AROMATIQUES BICYCLIQUES AMINOMETHYLE SUBSTITUES PERMETTANT DE TRAITER DES TROUBLES REPONDANT A UNE MODULATION DU RECEPTEUR D3 DE LA DOPAMINE
  申请人：ABBOTT GMBH & CO KG

  公开号：WO2006040180A1

  公开（公告）日：2006-04-20

  The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula (I) wherein Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered C-bound heteroaromatic radical comprising as ring member 1, 2 or 3 heteroatoms which are, independently of each other, selected from O, S and N, and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, O and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR8, where R8 is H, C1-C4-alkyl, fluorinated C1-C4-alkyl, C1-C4-alkylcarbonyl or fluorinated C1-C4-alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents Ra, wherein the variable Ra has the meanings given in the claims and in the description; X is a covalent bond or N-R2, CHR2, CHR2CH2, N or C-R2; Y is N-R2a, CHR2a, CHR2aCH2 or CHR2aCH2CH2; is a single bond or a double bond; E is CH2 or NR3; R1 is H, C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1­-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3­-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3­-C4-cycloalkyl, fluorinated C3-C4-alkenyl, R2 and R2a each independently are H, CH3, CH2F, CHF2 or CF3 or R1a and R2 or R1a and R2a together are (CH2)n with n being 1, 2 or 3; R3 is H or C1-C4-alkyl; R4 and R5 independently of each other are H, C1-C4-alkyl, fluorinated C1-C4-alkyl or C1-C4­-alkoxy or may form, together with N, a 4-, 5- or 6-membered saturated or unsaturated ring; R6 and R7 independently of each other are H or halogen; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

  本发明涉及一种氨甲基取代的双环芳香化合物，其化学式为(I)，其中Ar是从苯基、一个含有1、2或3个杂原子的5-或6成员C-键合杂芳基组成的环状基团中选择的循环基团，这些杂原子独立地选择自O、S和N，以及与饱和或不饱和的5-或6成员碳环或杂环融合的苯环，其中杂环包括作为环成员的1、2或3个选自N、O和S的杂原子和/或每个独立选择自NR8的1、2或3个含杂原子的基团，其中R8为H、C1-C4-烷基、氟代C1-C4-烷基、C1-C4-烷基酰基或氟代C1-C4-烷基酰基，环状基团Ar可能携带1、2或3个取代基Ra，其中变量Ra具有权利要求和描述中给定的含义；X是共价键或N-R2、CHR2、CHR2CH2、N或C-R2；Y是N-R2a、CHR2a、CHR2aCH2或CHR2aCH2CH2；是单键或双键；E是CH2或NR3；R1是H、C1-C4-烷基、C3-C4-环烷基、C3-C4-环烷基甲基、C3-C4-烯基、氟代C1-C4-烷基、氟代C3-C4-环烷基、氟代C3-C4-环烷基甲基、氟代C3-C4-烯基、甲酰基或C1-C3-烷基酰基；R1a是H、C1-C4-烷基、C3-C4-环烷基、C3-C4-烯基、氟代C1-C4-烷基、氟代C3-C4-环烷基、氟代C3-C4-烯基，R2和R2a各自独立地为H、CH3、CH2F、CHF2或CF3，或者R1a和R2或R1a和R2a一起为(CH2)n，其中n为1、2或3；R3为H或C1-C4-烷基；R4和R5独立地为H、C1-C4-烷基、氟代C1-C4-烷基或C1-C4-烷氧基，或者与N一起形成4、5或6成员饱和或不饱和环；R6和R7独立地为H或卤素；以及其生理耐受的酸盐加合物。该发明还涉及使用化合物(I)或其药学上可接受的盐制备用于治疗对多巴胺D3受体配体治疗敏感的医疗紊乱的药物组合物。
• Aminomethyl Substituted Bicyclic Aromatic Compounds Suitable for Treating Disorders That Respond to Modulation of the Dopamine D3 Receptor
  申请人：Drescher Karla

  公开号：US20110144146A1

  公开（公告）日：2011-06-16

  The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula I wherein Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered C-bound heteroaromatic radical comprising as ring member 1, 2 or 3 heteroatoms which are, independently of each other, selected from O, S and N, and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, 0 and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR 8 , where R 8 is H, C 1 -C 4 -alkyl, fluorinated C 1 -C 4 -alkyl, C 1 -C 4 -alkylcarbonyl or fluorinated C 1 -C 4 -alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents R a , wherein the variable R a has the meanings given in the claims and in the description; X is a covalent bond or N—R 2 , CHR 2 , CHR 2 CH 2 , N or C—R 2 ; Y is N—R 2a , CHR 2a , CHR 2a CH 2 or CHR 2a CH 2 CH 2 ; is a single bond or a double bond; E is CH 2 or NR 3 ; R 1 is H, C 3 -C 4 -cycloalkyl, C 3 -C 4 -cycloalkylmethyl, C 3 -C 4 -alkenyl, fluorinated C 1 -C 4 -alkyl, fluorinated C 3 -C 4 -cycloalkyl, fluorinated C 3 -C 4 -cycloalkylmethyl, fluorinated C 3 -C 4 -alkenyl, formyl or C 1 -C 3 -alkylcarbonyl; R 1a is H, C 1 C 4 -alkyl, C 3 -C 4 -cycloalkyl, C 3 -C 4 -alkenyl, fluorinated C 1 -C 4 -alkyl, fluorinated C 3 -C 4 -cycloalkyl, fluorinated C 3 -C 4 -alkenyl, R 2 and R 2a each independently are H, CH 3 , CH 2 F, CHF 2 or CF 3 or R 1a and R 2 or R 1a and R 2a together are (CH 2 ) n with n being 1, 2 or 3; R 3 is H or C 1 C 4 -alkyl; R 4 and R 5 independently of each other are H, C 1 -C 4 -alkyl, fluorinated C 1 -C 4 -alkyl or C 1 -C 4 -alkoxy or may form, together with N, a 4-, 5- or 6-membered saturated or unsaturated ring; R 6 and R 7 independently of each other are H or halogen; and the physiologically tolerated acid addition salts thereof.

  本发明涉及一种式子I的氨甲基取代的双环芳香化合物，其中Ar是从苯基、包含1、2或3个杂原子的5-或6元素C-键杂环基团（杂原子独立地选自O、S和N），以及与饱和或不饱和的5-或6元素碳环或杂环环融合的苯环，其中杂环环成员选自N、O和S和/或1、2或3个杂原子含量的基团，每个基团独立地选自NR8，其中R8是H、C1-C4-烷基、氟代C1-C4-烷基、C1-C4-烷基羰基或氟代C1-C4-烷基羰基，环状基团Ar可以携带1、2或3个取代基Ra，其中变量Ra的含义在权利要求和说明书中给出；X是共价键或N-R2、CHR2、CHR2CH2、N或C-R2；Y是N-R2a、CHR2a、CHR2aCH2或CHR2aCH2CH2；是单键或双键；E是CH2或NR3；R1是H、C3-C4-环烷基、C3-C4-环烷基甲基、C3-C4-烯基、氟代C1-C4-烷基、氟代C3-C4-环烷基、氟代C3-C4-环烷基甲基、氟代C3-C4-烯基、甲酰基或C1-C3-烷基羰基；R1a是H、C1-C4-烷基、C3-C4-环烷基、C3-C4-烯基、氟代C1-C4-烷基、氟代C3-C4-环烷基、氟代C3-C4-烯基，R2和R2a各自独立地为H、CH3、CH2F、CHF2或CF3，或者R1a和R2或R1a和R2a一起为(CH2)n，其中n为1、2或3；R3是H或C1-C4-烷基；R4和R5独立地为H、C1-C4-烷基、氟代C1-C4-烷基或C1-C4-烷氧基，或者可以与N一起形成4、5或6元素的饱和或不饱和环；R6和R7独立地为H或卤素；以及其生理耐受的酸加成盐。
• COMPOUNDS
  申请人：Barfoot Christopher

  公开号：US20100197679A1

  公开（公告）日：2010-08-05

  Bicyclic nitrogen containing compounds and their use as antibacterials

  双环氮含量化合物及其作为抗菌剂的使用
• Aminomethyl substituted bicyclic aromatic compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor
  申请人：Drescher Karla

  公开号：US08486984B2

  公开（公告）日：2013-07-16

  The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula I The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

  本发明涉及公式I的氨甲基取代的双环芳香化合物。本发明还涉及使用公式I的化合物或其药学上可接受的盐来制备用于治疗可用多巴胺D3受体配体治疗的医学疾患的制药组合物。
• AMINOMETHYL SUBSTITUTED BICYCLIC AROMATIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
  申请人：Abbott GmbH & Co. KG

  公开号：EP1809598A1

  公开（公告）日：2007-07-25