3-methyl-3-trifluoroacetamidoazetidine hydrochloride

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 3-methyl-3-trifluoroacetamidoazetidine hydrochloride
• 英文别名: 2,2,2-trifluoro-N-(3-methylazetidin-3-yl)acetamide;hydrochloride
• 化学式: C₆H₉F₃N₂O*ClH
• 分子量: 218.606
• InChiKey: RGNZSFXVBCYEPT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.45
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  41.1
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  6,7-二氟-1-(4-氟苯基)-4-氧代-1,4-二氢喹啉-3-羧酸 、 3-methyl-3-trifluoroacetamidoazetidine hydrochloride 在 三乙胺 作用下， 以 吡啶 为溶剂， 生成 1-(4-fluorophenyl)-6-fluoro-7-(3-amino-3-methyl-1-azetidinyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
  参考文献：
  名称：

  Derivatives of 7-(1-azetidinyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic

  摘要：

  本发明涉及新的杂环化合物，即7-(1-氮杂环丙基)-1,4-二氢-4-氧代-3-喹啉羧酸衍生物，其特征在于它们符合以下式（I）##STR1## 本发明还涉及这些化合物的制备以及它们作为药物的应用。

  公开号：

  US04927926A1

文献信息

• Substituted azetidinylpyridone naphthyridine carboxylic acid derivatives
  申请人：Laboratorios Del Dr. Esteve S.A.

  公开号：US05393758A1

  公开（公告）日：1995-02-28

  The present invention relates to new azetidine derivatives of substituted azetidinylpyridonecarboxylic acids, of 1,4-dihydro-4-oxo-3-quinolinecarboxylic, 4-oxo-1,8-naphthyridine-3-carboxylic and 2,3-dihydro-7-oxo-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acids, represented by the general formula I: ##STR1## The present invention also relates to therapeutically acceptable salts of these compounds, a process for preparing them and their application as medicinal products.

  本发明涉及代替的氮杂环吡啶酮羧酸的新型氮杂环衍生物，包括1,4-二氢-4-氧基-3-喹啉羧酸、4-氧基-1,8-萘啉并[3-羧酸和2,3-二氢-7-氧基-7H-吡啶并[1,2,3-de][1,4]苯并噁唑-6-羧酸，其通式为I：##STR1## 本发明还涉及这些化合物的治疗上可接受的盐，制备它们的方法以及它们作为药物的应用。
• 7-Azetidinylquinolones as antibacterial agents. Synthesis and structure-activity relationships
  作者：Jordi Frigola、Juan Pares、Jordi Corbera、David Vano、Ramon Merce、Antoni Torrens、Josep Mas、Eduard Valenti

  DOI：10.1021/jm00059a002

  日期：1993.4

  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.
• US4927926A
  申请人：——

  公开号：US4927926A

  公开（公告）日：1990-05-22
• US5395840A
  申请人：——

  公开号：US5395840A

  公开（公告）日：1995-03-07
• US5393758A
  申请人：——

  公开号：US5393758A

  公开（公告）日：1995-02-28