Tert-butyl 4-(1-chloro-2-(dimethylamino)ethylidene)piperidine-1-carboxylate | 849701-87-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: Tert-butyl 4-(1-chloro-2-(dimethylamino)ethylidene)piperidine-1-carboxylate
• 英文别名: tert-butyl 4-[1-chloro-2-(dimethylamino)ethylidene]piperidine-1-carboxylate
• CAS: 849701-87-7
• 化学式: C₁₄H₂₅ClN₂O₂
• 分子量: 288.818
• InChiKey: VNPJGMCXFMGBBA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.79
• 拓扑面积：
  32.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  Tert-butyl 4-(1-chloro-2-(dimethylamino)ethylidene)piperidine-1-carboxylate 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 生成 2-chloro-N,N-dimethyl-2-piperidin-4-ylideneethanamine
  参考文献：
  名称：

  7-(4-Alkylidenylpiperidinyl)-quinolone bacterial topoisomerase inhibitors

  摘要：

  Novel antibacterial fluoroquinolone agents bearing a 4-alkylidenylpiperidine 7-position substituent are active against quinolone-susceptible and quinolone-resistant gram-positive bacteria, including Streptococcus pneumoniae and MRSA. Analogs 22b, 23c, and 24 demonstrated superior in vitro and in vivo efficacy to ciprofloxacin against these cocci. (C) 2014 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2014.10.014
• 作为产物：
  描述：

  tert-butyl 4-(1-chloro-2-ethoxy-2-oxoethylidene)piperidine-1-carboxylate 在 二异丁基氢化铝 、 甲基磺酰氯 、 三乙胺 作用下， 以 四氢呋喃 、 二氯甲烷 、 乙腈 为溶剂， 生成 Tert-butyl 4-(1-chloro-2-(dimethylamino)ethylidene)piperidine-1-carboxylate
  参考文献：
  名称：

  7-(4-Alkylidenylpiperidinyl)-quinolone bacterial topoisomerase inhibitors

  摘要：

  Novel antibacterial fluoroquinolone agents bearing a 4-alkylidenylpiperidine 7-position substituent are active against quinolone-susceptible and quinolone-resistant gram-positive bacteria, including Streptococcus pneumoniae and MRSA. Analogs 22b, 23c, and 24 demonstrated superior in vitro and in vivo efficacy to ciprofloxacin against these cocci. (C) 2014 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2014.10.014

文献信息

• 7-AMINO ALKYLIDENYL-HETEROCYCLIC QUINOLONES AND NAPHTHYRIDONES
  申请人：Davis Benjamin

  公开号：US20090156577A1

  公开（公告）日：2009-06-18

  The present invention relates to compounds having a structure according to Formula (I) wherein n, m, z, R, R 2 , R 3 , R 4 , R 5 , R 6 , A, E, X, Y, a and b are as defined above; or an optical isomer, diastereomer or enantiomer thereof; a pharmaceutically acceptable salt, hydrate, or prodrug thereof.

  本发明涉及具有以下公式(I)结构的化合物，其中n、m、z、R、R2、R3、R4、R5、R6、A、E、X、Y、a和b如上定义；或其光学异构体、对映异构体或差向异构体；其药学上可接受的盐、水合物或前药。
• US7179805B2
  申请人：——

  公开号：US7179805B2

  公开（公告）日：2007-02-20
• US7732612B2
  申请人：——

  公开号：US7732612B2

  公开（公告）日：2010-06-08
• [EN] 7-AMINO ALKYLIDENYL-HETEROCYCLIC QUINOLONES AND NAPHTHYRIDONES<br/>[FR] QUINOLONES ET NAPHTYRIDONES 7-AMINO-ALKYLIDÉNYL-HÉTÉROCYCLIQUES
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2010056633A2

  公开（公告）日：2010-05-20

  The present invention relates to compounds having a structure according to Formula (I) R4 o o Ra R A" 6 Y Formula (I) wherein n, m, z, R, R2, R3, R4, R5, Re, A, E, X, Y, a and b are as defined above; or an optical isomer, diastereomer or enantiomer thereof; a pharmaceutically acceptable salt, hydrate, or prodrug thereof.
• 7-(4-Alkylidenylpiperidinyl)-quinolone bacterial topoisomerase inhibitors
  作者：Eugene B. Grant、Barbara D. Foleno、Raul Goldschmidt、Jamese J. Hilliard、Shu-Chen Lin、Brian Morrow、Steven D. Paget、Michele A. Weidner-Wells、Xiaodong Xu、Xiaoqing Xu、William V. Murray、Karen Bush、Mark J. Macielag

  DOI：10.1016/j.bmcl.2014.10.014

  日期：2014.12

  Novel antibacterial fluoroquinolone agents bearing a 4-alkylidenylpiperidine 7-position substituent are active against quinolone-susceptible and quinolone-resistant gram-positive bacteria, including Streptococcus pneumoniae and MRSA. Analogs 22b, 23c, and 24 demonstrated superior in vitro and in vivo efficacy to ciprofloxacin against these cocci. (C) 2014 Elsevier Ltd. All rights reserved.