6-Propyl-5,5a,6,7,8,9,9a,10-octahydropyrido[2,3-g]quinazolin-2-amine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 6-Propyl-5,5a,6,7,8,9,9a,10-octahydropyrido[2,3-g]quinazolin-2-amine
• 英文别名: 6-propyl-5a,7,8,9,9a,10-hexahydro-5H-pyrido[2,3-g]quinazolin-2-amine
• 化学式: C₁₄H₂₂N₄
• 分子量: 246.35
• InChiKey: TUFADSGTJUOBEH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  55
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Pyrimido(4,5-g)quinolines, process for their preparation, and pharmaceutical compositions containing them
  申请人：ELI LILLY AND COMPANY

  公开号：EP0139393A2

  公开（公告）日：1985-05-02

  Trans-(±)-2-Amino (or substituted amino)-4-(permissibly-substituted)-6-C1-C3 alkyl (or allyl)-5,5a,-6,7,8,9,9a,10-octahydropyrimido[4,5-g]quinolines, the corresponding trans-(-) and trans-(+)-stereoisomers and salts thereof, useful in treating Parkinson's Syndrome, sexual dysfunction, depression, hypertension, and prolactin related diseases, and intermediates useful for the synthesis thereof, are disclosed. The products are prepared by condensing an appropriate ketone with the appropriately substituted guanidine.

  本发明涉及转型-(±)-2-氨基(或取代氨基)-4-(可取代基)-6-C1-C3烷基(或烯丙基)-5,5a,-6,7,8,9,9a,10-八氢嘧啶[4,5-g]喹啉，相应的转型-(-)和转型-(+)-立体异构体及其盐，用于治疗帕金森综合症、性功能障碍、抑郁症、高血压和催乳素相关疾病，以及用于其合成的中间体。所述产品通过将适当的酮与适当取代的胍缩合制备而成。
• Improvements in or relating to tricycling quinoline derivatives
  申请人：ELI LILLY AND COMPANY

  公开号：EP0171277A2

  公开（公告）日：1986-02-12

  A process for preparing trycyclic quinoline derivatives having dopamine agonist properties by reducing the corresponding lactam precursors.

  一种通过还原相应的内酰胺前体制备具有多巴胺激动剂特性的试环喹啉衍生物的工艺。
• Synthesis of 2-aminopyrimido [4,5-g] quinolines
  申请人：ELI LILLY AND COMPANY

  公开号：EP0241186A1

  公开（公告）日：1987-10-14

  This invention provides a process for prepar­ing trans 2-aminopyrimido[4,5-g]quinolines of formula wherein R is hydrogen, cyano, C₁-C₃ alklyl or allyl; R¹ is amino, -NHR³ or -NR⁴R⁵; R² is hydrogen or methyl; R³ is methyl, ethyl, n-propyl, C₁-C₃ alkyl-CO, phenyl-CO or substituted phenyl-CO, wherein said substituents are 1 or 2 members selected from the group consisting of chloro, fluoro, bromo, methyl, ethyl, methoxy, ethoxy and trifluoromethyl; and R⁴ and R⁵ are individually methyl, ethyl or n-propyl, which comprises reacting a compound of the formula wherein R⁶ is C₁-C₃ alkyl, phenyl, 4-chlorophenyl, 4-bromophenyl or 4-methylphenyl, with a guanidine salt. The compounds are dopamine agonists.

  本发明提供了一种制备反式 2-氨基嘧啶并[4,5-g]喹啉的工艺，其式为 其中 R 是氢、氰基、C₁-C₃ 烷基或烯丙基；R¹ 是氨基、-NHR³ 或 -NR⁴R⁵ ；R² 是氢或甲基；R³ 是甲基、乙基、正丙基、C₁-C₃ 烷基-CO、苯基-CO 或取代苯基-CO，其中所述取代基为 1 或 2 个选自氯、氟、溴、甲基、乙基、甲氧基、乙氧基和三氟甲基组成的组的成员；以及 R⁴ 和 R⁵ 单独是甲基、乙基或正丙基。 其中 R⁶ 是 C₁-C₃ 烷基、苯基、4-氯苯基、4-溴苯基或 4-甲基苯基，与胍盐反应。这些化合物是多巴胺激动剂。
• EP0139393B1
  申请人：——

  公开号：EP0139393B1

  公开（公告）日：1991-05-15
• Treatment of fibromyalgia and chronic fatigue syndrome
  申请人：——

  公开号：US20030212085A1

  公开（公告）日：2003-11-13

  The present invention relates to the treatment of neuromuscular disorders and, more specifically, to the use of apomorphine, bromocriptine, pergolide, ropinirole, octahydropyrazolo[3,4-g]quinolines, and trans-(±)-substituted-5,5a,6,7,8,9-,9a,10-octahydropyrimido[4,5g]quinolines, and their pharmaceutically acceptable salts to treat, or to prepare a medicament for treating, symptoms of fibromyalgia syndrome and chronic fatigue syndrome.