N-[3-(quinolin-7-yloxy)propyl]-2,3-dihydro-6,7-methylenedioxy-1,4-benzodioxin-2-methanamine | 151450-57-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: N-[3-(quinolin-7-yloxy)propyl]-2,3-dihydro-6,7-methylenedioxy-1,4-benzodioxin-2-methanamine
• 英文别名: N-(6,7-dihydro-[1,3]dioxolo[4,5-g][1,4]benzodioxin-6-ylmethyl)-3-quinolin-7-yloxypropan-1-amine
• CAS: 151450-57-6
• 化学式: C₂₂H₂₂N₂O₅
• 分子量: 394.427
• InChiKey: SVIQNLDNGHRSSC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  29
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  71.1
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  2,3-Dihydro-6,7-methylenedioxy-1,4-benzodioxin-2-methanamine 、 7-(3-bromopropoxy)quinoline 、 N,N-二异丙基乙胺 、 碘化钠 在 氮气 、 碳酸氢钠 、 氯化钠 、 Sodium sulfate-III 、 silica gel 、 residue 、 乙醇 、 盐酸 、 hydron;2,4,5,6-tetrafluorobenzene-1,3-diamine;dichloride 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 15.0h， 以to give 1.25 g of the title compound as a yellow solid dihydrochloride salt, m.p. 224°-226° C.的产率得到N-[3-(quinolin-7-yloxy)propyl]-2,3-dihydro-6,7-methylenedioxy-1,4-benzodioxin-2-methanamine
  参考文献：
  名称：

  Antipsychotic quinoline derivatives of benzodioxanmethylamine

  摘要：

  该化合物的化学式为：##STR1## 其中R.sup.1和R.sup.2分别为氢，烷基，烷氧基，芳基烷氧基，脂肪酰氧基，羟基，卤素，氨基，单烷基或二烷基氨基，脂肪酰胺基或磺酰胺基，或R.sup.1和R.sup.2在一起为亚甲二氧基，乙二氧基或丙二氧基; R.sup.3为氢或烷基; n为整数2、3或4; 或其药学上可接受的盐，均为抗精神病药物。

  公开号：

  US05235055A1

文献信息

• Antipsychotic quinoline derivatives of benzodioxanmethylamine
  申请人：American Home Products Corporation

  公开号：US05235055A1

  公开（公告）日：1993-08-10

  A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, alkanamido or sulfonamido, or R.sup.1 and R.sup.2 together are methylenedioxy, ethylenedioxy or propylenedioxy; R.sup.3 is hydrogen or alkyl; n is one of the integers 2, 3 or 4; or a pharmaceutically acceptable salt thereof, are antipsychotic agents.

  该化合物的化学式为：##STR1## 其中R.sup.1和R.sup.2分别为氢，烷基，烷氧基，芳基烷氧基，脂肪酰氧基，羟基，卤素，氨基，单烷基或二烷基氨基，脂肪酰胺基或磺酰胺基，或R.sup.1和R.sup.2在一起为亚甲二氧基，乙二氧基或丙二氧基; R.sup.3为氢或烷基; n为整数2、3或4; 或其药学上可接受的盐，均为抗精神病药物。
• ANTIPSYCHOTIC QUINOLINE DERIVATIVES OF BENZODIOXANMETHYLAMINE
  申请人：AMERICAN HOME PRODUCTS CORPORATION

  公开号：EP0658160A1

  公开（公告）日：1995-06-21
• Combination of a dopamine D2-receptor agonist and tiotropium or a derivative therof for treating obstructive airways and other inflammatory diseases
  申请人：Yeadon Michael

  公开号：US20070117788A1

  公开（公告）日：2007-05-24

  The present invention relates to a combination of therapeutic agents useful in the treatment of obstructive airways and other inflammatory diseases comprising (I) a dopamine D2-receptor agonist that is therapeutically effective in the treatment of said diseases when administered by inhalation; together with (II) an anti-cholinergic agent consisting of a member selected from the group consisting of tiotropium and derivatives thereof that is therapeutically effective in the treatment of said diseases when administered by inhalation; as well as to a method of treating said obstructive airways and other inflammatory diseases comprising administering to said mammal by inhalation a therapeutically effective amount of said combination of therapeutic agents; and a pharmaceutical composition comprising a pharmaceutically acceptable carrier together with said combination of therapeutic agents; and a package containing a pharmaceutical composition for insertion into a device capable of simultaneous or sequential delivery of said pharmaceutical composition in the form of an aerosol or dry powder dispersion to said mammal, where said device is a metered dose inhaler or a dry powder inhaler. It is preferred that said dopamine D2-receptor agonist component be bromocriptine mesylate, naxagolide hydrochloride, cabergoline, pergolide mesylate, quinpirole hydrochloride, or ropinirole hydrochloride; and that said anti-cholinergic agent component be tiotropium bromide.
• US5235055A
  申请人：——

  公开号：US5235055A

  公开（公告）日：1993-08-10
• [EN] ANTIPSYCHOTIC QUINOLINE DERIVATIVES OF BENZODIOXANMETHYLAMINE<br/>[FR] DERIVES QUIOLINIQUES DE BENZODIOXANMETHYLAMINE NEUROLEPTIQUES
  申请人：——

  公开号：WO1994005655A1

  公开（公告）日：1994-03-17

  [EN] A compound of formula (1), wherein R1 and R2 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, alkanamido or sulfonamido, or R1 and R2 together are methylenedioxy, ethylenedioxy or propylenedioxy; R3 is hydrogen or alkyl; n is one of the integers 2, 3 or 4; or a pharmaceutically acceptable salt thereof, are antipsychotic agents.
  [FR] Cette invention concerne un composé de formule (1) dans lequel R1 et R2 représentent indépendamment hydrogène, alkyle, alcoxy, aralcoxy, alcanoyloxy, hydroxy, halo, amino, mono- ou dialkylamino, alcanamido ou sulfonamido, ou bien R1 et R2 représentent ensemble méthylènedioxy, éthylènedioxy ou propylènedioxy; R3 représente hydrogène ou alkyle; et n représente un entier tel que 2, 3 ou 4. Ce composé ou un de ses sels pharmaceutiquement acceptable est un neuroleptique.