1-(二苯基甲基)-N,3-二甲基-3-氮杂环丁胺 | 133891-60-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 1-(二苯基甲基)-N,3-二甲基-3-氮杂环丁胺
• 英文名称: 1-(diphenylmethyl)-3-methyl-3-methylaminoazetidine
• 英文别名: 1-(Diphenylmethyl)-N,3-dimethylazetidin-3-amine；1-benzhydryl-N,3-dimethylazetidin-3-amine
• CAS: 133891-60-8
• 化学式: C₁₈H₂₂N₂
• 分子量: 266.386
• InChiKey: PVQXRYTXOATJFJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  15.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-(二苯基甲基)-N,3-二甲基-3-氮杂环丁胺 、 三氟乙酸酐 以 氯仿 为溶剂， 反应 2.0h， 生成 1-(diphenylmethyl)-3-methyl-3-azetidine
  参考文献：
  名称：

  7-Azetidinylquinolones as antibacterial agents. Synthesis and structure-activity relationships

  摘要：

  A series of novel antibacterial quinolones and naphthyridones has been prepared which contain 7-azetidinyl substituents in place of the usual piperazine or aminopyrrolidine groups. These azetidinyl derivatives were evaluated for in vitro activity by determining minimum inhibitory concentrations against a variety of bacteria. In vivo efficacy in the mouse infection model and blood levels in the mouse were determined for several compounds. The influence on the structure-activity relationships of varying substituents in the azetidine ring and at position 8 (CH, CF, CCl, N) and N-1 (ethyl, fluoroethyl, cyclopropyl, tert-butyl, 4-fluorophenyl, and 2,4-difluorophenyl) was also studied. Compounds with outstandingly broad-spectrum activity, particularly against Gram-positive organisms, improved in vivo efficacy, and high blood levels were identified in this work. 7-Azetidinyl-8-chloroquinolones were considered as warranting further development.

  DOI：

  10.1021/jm00059a002
• 作为产物：
  描述：

  1-(二苯基甲基)-3-甲基-3-羟基氮杂啶 在 三乙胺 作用下， 以 二氯甲烷 、 异丙醇 为溶剂， 反应 3.0h， 生成 1-(二苯基甲基)-N,3-二甲基-3-氮杂环丁胺
  参考文献：
  名称：

  7-Azetidinylquinolones as antibacterial agents. Synthesis and structure-activity relationships

  摘要：

  A series of novel antibacterial quinolones and naphthyridones has been prepared which contain 7-azetidinyl substituents in place of the usual piperazine or aminopyrrolidine groups. These azetidinyl derivatives were evaluated for in vitro activity by determining minimum inhibitory concentrations against a variety of bacteria. In vivo efficacy in the mouse infection model and blood levels in the mouse were determined for several compounds. The influence on the structure-activity relationships of varying substituents in the azetidine ring and at position 8 (CH, CF, CCl, N) and N-1 (ethyl, fluoroethyl, cyclopropyl, tert-butyl, 4-fluorophenyl, and 2,4-difluorophenyl) was also studied. Compounds with outstandingly broad-spectrum activity, particularly against Gram-positive organisms, improved in vivo efficacy, and high blood levels were identified in this work. 7-Azetidinyl-8-chloroquinolones were considered as warranting further development.

  DOI：

  10.1021/jm00059a002

文献信息

• 4-AMINOPYRIMIDINE DERIVATIVES AS HISTAMINE H4 RECEPTOR ANTAGONISTS
  申请人：Carceller González Elena

  公开号：US20110039817A1

  公开（公告）日：2011-02-17

  4-Aminopyrimidine derivatives of formula (I) that are useful as histamine H4 receptor antagonists.

  式(I)的4-氨基嘧啶衍生物可用作组胺H4受体拮抗剂。
• 1-Benzhydrylazétidines, leur préparation et leur application comme intermédiaires pour la préparation de composés à activité antimicrobienne
  申请人：LABORATORIOS DEL DR. ESTEVE, S.A.

  公开号：EP0406112A1

  公开（公告）日：1991-01-02

  Nouvelles azétidines caractérisées en ce qu'elles répondent à la formule générale (I) dans laquelle R₃ représente un radical amino, un radical alkylamino, un radical cycloalkylamino, un radical acylamino, un radical alkylacylamino, un radical aminométhyle, un radical alkylaminométhyle, un radical acylaminométhyle, ou un radical alkylacyl­aminométhyle, dans lesquels chaque fragment acyle peut être substitué par un ou plusieurs atomes d'halogène, en particulier de fluor ; R₁, R₂, R₄, R₅ et R₆ représentent un atome d'hydrogène ou un radical alkyle inférieure, avec la condition que au moins un d'eux représente un radical alkyle inférieure, ainsi que leurs sels.

  新型氮杂环丁烷，其特征在于它们符合通式 (I) 其中 R₃ 代表氨基基、烷基氨基基、环烷基氨基基、酰氨基基、烷基酰氨基基、氨基甲基基、烷基氨基甲基基、酰氨基甲基基或烷基酰氨基甲基基，其中每个酰基可被一个或多个卤素原子取代，特别是氟； R₁、R₂、R₄、R₅ 和 R₆ 代表氢原子或低级烷基，但其中至少有一个代表低级烷基，以及它们的盐。
• US5073646A
  申请人：——

  公开号：US5073646A

  公开（公告）日：1991-12-17
• US8431580B2
  申请人：——

  公开号：US8431580B2

  公开（公告）日：2013-04-30