(R)-6-溴-2-氨基四啉 | 167172-92-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 中文名称: (R)-6-溴-2-氨基四啉
• 英文名称: (r)-6-Bromo-2-aminotetralin
• 英文别名: (2R)-6-bromo-1,2,3,4-tetrahydronaphthalen-2-amine
• CAS: 167172-92-1
• 化学式: C₁₀H₁₂BrN
• 分子量: 226.11
• InChiKey: WMALPFDUOAVVMB-SNVBAGLBSA-N

物化性质

• 沸点：
  298.7±40.0 °C(Predicted)
• 密度：
  1.413±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 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：
  26
• 氢给体数：
  1
• 氢受体数：
  1

安全信息

• 海关编码：
  2921450090

反应信息

• 作为反应物：
  描述：

  二碳酸二叔丁酯 、 (R)-6-溴-2-氨基四啉 、 三乙胺 在 水 、 Sodium sulfate-III 作用下， 以 N,N-二甲基甲酰胺 、 ethyl acetate n-hexane 为溶剂， 反应 3.0h， 生成 ((R)-6-bromo-1,2,3,4-tetrahydro-naphthalen-2-yl)-carbamic acid tert-butyl ester
  参考文献：
  名称：

  Piperazine derivatives and methods of use

  摘要：

  所选化合物对于治疗疼痛和炎症介导的疾病有效。本发明包括新型化合物、类似物、前药和其药学上可接受的衍生物、药物组合物以及预防和治疗涉及疼痛、炎症等疾病和其他不适或病症的方法。本发明还涉及制造这些化合物的工艺以及在这些工艺中有用的中间体。

  公开号：

  US07393852B2

文献信息

• [EN] ARYLSULFONYLMETHYL OR ARYLSULFONAMIDE SUBSTITUTED AROMATIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MADULATION OF THE DOPAMINE D3 RECEPTOR<br/>[FR] COMPOSES AROMATIQUES D'ARYLSULFONYLMETHYLE OU D'ARYLSULFONAMIDE 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：WO2006040178A1

  公开（公告）日：2006-04-20

  The present invention relates to aromatic compounds of the formula (I), wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; Y is O, S, -CH=N-, -CH=CH- or -N=CH-; A is CH2i O or S; E is CR6R7 or NR 3; R1 is 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 C,-C3-alkylcarbonyl; R1a is H, C2-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4 -cycloalkyl, or R1a and R2 together are (CH2)n with n being 2 or 3, or R1a and R2a together are (CH2)n with n being 2 or 3; R2 and R2a are independently of each other H, CH3, CH2F, CHF2 or CF3; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, C1-C2-alkyl and fluorinated C1-C2-alkyl; 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.

  本发明涉及式(I)的芳香族化合物，其中Ar是苯基或芳香族5-或6-成员C-键合杂芳基，其中Ar可以携带1个基团Ra，Ar也可以携带1个或2个基团Rb；X是N或CH；Y是O、S、-CH=N-、-CH=CH-或-N=CH-；A是CH2i、O或S；E是CR6R7或NR3；R1是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C,-C3-烷基羰基；R1a是H、C2-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，或R1a和R2一起是(CH2)n，其中n为2或3，或R1a和R2a一起是(CH2)n，其中n为2或3；R2和R2a彼此独立地是H、CH3、CH2F、CHF2或CF3；R3是H或C1-C4-烷基；R6、R7彼此独立地选自H、C1-C2-烷基和氟代C1-C2-烷基；以及其生理耐受的酸盐。该发明还涉及使用式I的化合物或其药学上可接受的盐制备用于治疗对多巴胺D3受体配体敏感的医疗疾病的药物组合物。
• Process for preparation of 2-aminotetralin derivatives and intermediates thereof
  申请人：Honda Tatsuya

  公开号：US20050153408A1

  公开（公告）日：2005-07-14

  The present invention is to efficiently and simply prepare an optically active 7-substituted-2-aminotetralin with industrial advantage. In the process, a 7-substituted-2-tetralone or its bisulfite adduct is reduced with a microorganism to an optically active 7-substituted-2-tetralol. Then, a sulfonyl group is introduced to the hydroxy group to form an optically active 7-substituted-2-sulfonyloxytetralin. Then, with inversion of the configuration, a nitrogen substituent is introduced using a nitrogen nucleophile to form an optically active 2,7-substituted tetralin. Furthermore, if necessary, the nitrogen substituent is converted into a non-substituted amino group. Thus, an optically active 7-substituted-2-aminotetralin or its salt is prepared.

  本发明旨在以工业优势高效简便地制备光学活性的7-取代-2-氨基四氢萘。在该过程中，使用微生物将7-取代-2-四氢萘酮或其亚硫酸盐加合物还原为光学活性的7-取代-2-四氢萘醇。然后，引入磺酰基到羟基上，以形成光学活性的7-取代-2-磺酰氧基四氢萘。接着，通过构型反演，使用氮亲核试剂引入氮取代基，以形成光学活性的2,7-取代四氢萘。此外，如有必要，氮取代基可转化为非取代的氨基。因此，制备了光学活性的7-取代-2-氨基四氢萘或其盐。
• Arylsulfonylmethyl or arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to modulation of the Dopamine D3 receptor
  申请人：Drescher Karla

  公开号：US20090012074A1

  公开（公告）日：2009-01-08

  The present invention relates to aromatic compounds of the formula I wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical R a and wherein Ar may also carry 1 or 2 radicals R b ; X is N or CH; Y is O, S, —CH═N—, —CH═CH— or —N═CH—; A is CH 2 , O or S; E is CR 6 R 7 or NR 3 ; R 1 is C 1 -C 4 -alkyl, 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 2 -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, or R 1a and R 2 together are (CH 2 ) n with n being 2 or 3, or R 1a and R 2a together are (CH 2 ) n with n being 2 or 3; R 2 and R 2a are independently of each other H, CH 3 , CH 2 F, CHF 2 or CF 3 ; R 3 is H or C 1 -C 4 -alkyl; R 6 , R 7 independently of each other are selected from H, C 1 -C 2 -alkyl and fluorinated C 1 -C 2 -alkyl; 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.

  本发明涉及公式I的芳香族化合物，其中Ar是苯基或含有5或6个成员的芳香族C-连接杂环基团，其中Ar可以携带1个基团Ra，也可以携带1或2个基团Rb；X是N或CH；Y是O，S，-CH═N-，-CH═CH-或-N═CH-；A是CH2，O或S；E是CR6R7或NR3；R1是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烷基羰基；R1a是H，C2-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，或R1a和R2一起是(CH2)n，其中n为2或3，或R1a和R2a一起是(CH2)n，其中n为2或3；R2和R2a相互独立地是H，CH3，CH2F，CHF2或CF3；R3是H或C1-C4烷基；R6，R7相互独立地选择自H，C1-C2烷基和氟代C1-C2烷基；以及其生理耐受酸盐。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制备用于治疗可通过多巴胺D3受体配体治疗的医疗障碍的制药组合物的用途。
• COMPOUNDS AND METHODS OF USE
  申请人：Groneberg Robert D.

  公开号：US20090048224A1

  公开（公告）日：2009-02-19

  Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  所选化合物可有效治疗疼痛和疾病，如炎症介导的疾病。该发明涵盖了新颖的化合物、类似物、前药和其药学上可接受的衍生物、制药组合物以及预防和治疗涉及疼痛、炎症等疾病和其他病症或状况的方法。该发明还涉及制备此类化合物的方法以及在这些过程中有用的中间体。
• 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