OCTAHYDROCYCLOPENTAL C PYRROL-5-AMINE | 130657-51-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: OCTAHYDROCYCLOPENTAL C PYRROL-5-AMINE
• 英文别名: (3aR,5R,6aS)-(Octahydro-cyclopenta[c]pyrrol-5-yl)amine
• CAS: 130657-51-1
• 化学式: C₇H₁₄N₂
• 分子量: 126.202
• InChiKey: ZTUKAUIYRJDBME-KVSKUHBBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.06
• 重原子数：
  9.0
• 可旋转键数：
  0.0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  38.05
• 氢给体数：
  2.0
• 氢受体数：
  2.0

反应信息

• 作为反应物：
  描述：

  1-环丙基-6,7,8-三氟-4-氧代-1,4-二氢喹啉-3-羧酸 、 OCTAHYDROCYCLOPENTAL C PYRROL-5-AMINE 在 1,8-二氮杂双环[5.4.0]十一碳-7-烯 作用下， 以 乙腈 为溶剂， 反应 4.0h， 生成 7-<7-amino-3-azabicyclo<3.3.0>octan-3-yl>-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
  参考文献：
  名称：

  Synthesis and antibacterial activity of new 7-(aminoazabicycloalkanyl)quinolonecarboxylic acids

  摘要：

  A series of novel 7-[amino-substituted azabicycloalkanyl]-6-fluoro-1-substituted quinolinecarboxylic acids (18-53) have been prepared and their antibacterial activities evaluated. These compounds are characterized structurally by a new amino-substituted azabicyclo[3.3.0]octane,-[4.3.0]nonane and -[5.3.0]decane ring systems at the 7-position of quinolonecarboxylic acids. To compare the biological activities of enantiomers, (+)-7[(1S, 5R)- and (-)-7[(1R, 5S)-1-aminomethyl-3-azabicyclo[3.3.0]-octan-3-yl]-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolonecarboxylic acid hydrochloride (43, 44) were synthesized and evaluated for antibacterial activity. Compound 43 was more potent than 44 against both Gram-positive and Gram-negative organisms. The structure-activity relationships of these quinolonecarboxylic acids are also discussed.

  DOI：

  10.1016/0223-5234(91)90131-6
• 作为产物：
  描述：

  (3aS,6aR)-benzyl 4-oxohexahydrocyclopenta[c]pyrrole-2(1H)-carboxylate 在 palladium on activated charcoal 四氯化碳 、 sodium azide 、 氰化钠 、 氢气 、 L-Selectride 、 三苯基膦 作用下， 以 四氢呋喃 、 甲醇 、 六甲基磷酰三胺 、 水 、 二甲基亚砜 、 N,N-二甲基甲酰胺 为溶剂， -78.0~140.0 ℃ 、506.62 kPa 条件下， 反应 12.0h， 生成 OCTAHYDROCYCLOPENTAL C PYRROL-5-AMINE
  参考文献：
  名称：

  Synthesis and antibacterial activity of new 7-(aminoazabicycloalkanyl)quinolonecarboxylic acids

  摘要：

  A series of novel 7-[amino-substituted azabicycloalkanyl]-6-fluoro-1-substituted quinolinecarboxylic acids (18-53) have been prepared and their antibacterial activities evaluated. These compounds are characterized structurally by a new amino-substituted azabicyclo[3.3.0]octane,-[4.3.0]nonane and -[5.3.0]decane ring systems at the 7-position of quinolonecarboxylic acids. To compare the biological activities of enantiomers, (+)-7[(1S, 5R)- and (-)-7[(1R, 5S)-1-aminomethyl-3-azabicyclo[3.3.0]-octan-3-yl]-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolonecarboxylic acid hydrochloride (43, 44) were synthesized and evaluated for antibacterial activity. Compound 43 was more potent than 44 against both Gram-positive and Gram-negative organisms. The structure-activity relationships of these quinolonecarboxylic acids are also discussed.

  DOI：

  10.1016/0223-5234(91)90131-6

文献信息

• DIHYDROPTERIDINONE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
  申请人：Jiangsu Hengrui Medicine Co., Ltd.

  公开号：EP2481739A1

  公开（公告）日：2012-08-01

  Dihydroperidinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specially, new dihydroperidinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is defined as in the description, their preparation process, pharmaceutical compositions comprising said derivatives and their use as therapeutical agents, especially as Plk kinase inhibitors are disclosed.

  本发明公开了二氢佩里酮衍生物、其制备工艺和药物用途。特别是，本发明公开了由通式（I）代表的新的二氢佩里酮衍生物（其中通式（I）的每个取代基定义如描述中所示）、它们的制备工艺、包含所述衍生物的药物组合物以及它们作为治疗剂，特别是作为 Plk 激酶抑制剂的用途。
• HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS, COMPOSITIONS COMPRISING THE HETEROCYCLIC COMPOUND, AND METHODS OF USE THEREOF
  申请人：JS Innopharm (Shanghai) Ltd

  公开号：US20220220128A1

  公开（公告）日：2022-07-14

  (I) Disclosed herein are compounds of formula I, and/or a stereoisomer, a stable isotope, or a pharmaceutically acceptable salt or solvate thereof; and therapeutic uses of these compounds, which are inhibitors of rearranged during transfection (RET), potentially useful in the treatment of RET-associated diseases, such as RET-associated cancers.