1-(2-amino-4-methoxyphenyl)-2-methylpropanone | 91099-20-6

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-(2-amino-4-methoxyphenyl)-2-methylpropanone
• 英文别名: 2-amino-4-methoxyisobutyrophenone；1-(2-Amino-4-methoxyphenyl)-2-methylpropan-1-one
• CAS: 91099-20-6
• 化学式: C₁₁H₁₅NO₂
• 分子量: 193.246
• InChiKey: QOBKDCHHSWDHPJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  52.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  1-(3-甲氧基苯基)脲 在 吡啶 、 PPA 、 Polyphosphoric acid (PPA) 作用下， 以 乙酸乙酯 、 苯 为溶剂， 反应 3.0h， 生成 1-(2-amino-4-methoxyphenyl)-2-methylpropanone
  参考文献：
  名称：

  Heinicke, Grant; Hung, Tran V.; Prager, Rolf H., Australian Journal of Chemistry, 1984, vol. 37, # 4, p. 831 - 844

  摘要：

  DOI：

文献信息

• Camptothecin derivatives and process for preparing same
  申请人：KABUSHIKI KAISHA YAKULT HONSHA

  公开号：EP0325247A1

  公开（公告）日：1989-07-26

  New camptothecin derivatives and a process for preparing same are disclosed, which are represented by the general formula: wherein R¹ represents a lower alkyl group, R² represents a hydrogen atom or an amino, hydroxyl, lower acylamino or lower alkoxy group, R³ represents a hydrogen or halogen atom or a lower alkyl, hydroxyl, lower alkoxy, nitro, amino, cyano or di(lower alkyl)amino group, R⁴ represents a hydrogen or halogen atom or a lower alkyl, hydroxyl, lower alkoxy, lower alkylthio, amino, cyano or di(lower alkyl)amino group, and R⁵ represents a hydrogen or halogen atom or a hydroxyl or lower alkoxy group, with the proviso that all of the R², R³, R⁴ and R⁵ substituents should not be a hydrogen atom and also that if any one of the R², R³, R⁴ and R⁵ is a hydroxyl or lower alkoxy group, all of the other three substituents should not be a hydrogen atom. The new camptothecin derivatives are useful as anti-tumor drugs or intermediates therefor.

  本发明公开了新喜树碱衍生物及其制备方法，它们由通式表示： 其中 R¹ 代表低级烷基，R² 代表氢原子或氨基、羟基、低级酰氨基或低级烷氧基，R³ 代表氢原子或卤素原子或低级烷基、羟基、低级烷氧基、硝基、氨基、氰基或二（低级烷基）氨基，R⁴ 代表氢原子或卤素原子或低级烷基、羟基、低级烷氧基、低级烷硫基、氨基、氰基或二（低级烷基）氨基，以及 R⁵ 代表氢原子或卤素原子或低级烷基、羟基、低级烷氧基、低级烷硫基、氨基、氰基或二（低级烷基）氨基、R⁴代表氢原子、卤素原子或低级烷基、羟基、低级烷氧基、低级烷硫基、氨基、氰基或二（低级烷基）氨基，R⁵代表氢原子、卤素原子或羟基或低级烷氧基，但所有 R²、R³、R⁴ 和 R⁵ 取代基都不能是氢原子，而且如果 R²、R³、R⁴ 和 R⁵ 中的任何一个是羟基或低级烷氧基，则其他三个取代基都不能是氢原子。新喜树碱衍生物可用作抗肿瘤药物或其中间体。
• HEINICKE, G.;HUNG, T. V.;PRAGER, R. H.;WARD, A. D., AUSTRAL. J. CHEM., 1984, 37, N 4, 831-844
  作者：HEINICKE, G.、HUNG, T. V.、PRAGER, R. H.、WARD, A. D.

  DOI：——

  日期：——
• BENZAMIDE INHIBITORS OF BACTERIAL LIPOPROTEIN SIGNAL PEPTIDASE
  申请人：The Scripps Research Institute

  公开号：US20200181101A1

  公开（公告）日：2020-06-11

  Increasing resistance to antibiotics necessitates discovery of new targets and strategies to combat bacteria. Ideal protein targets are required for viability across many species, are unique to prokaryotes to limit effects on the host and have robust assays to quantitate activity and identify novel inhibitors. Lipoprotein signal peptidase (Lsp) is a transmembrane aspartyl protease required for lipoprotein maturation and entirely fits these criteria. We have developed the first in vitro high-throughput assay to monitor proteolysis by Lsp. We employed our HTS assay against 646,275 compounds to discover inhibitors of Lsp and synthesized a range of analogues to generate molecules with nanomolar IC50 values. Importantly, our inhibitors are effective in preventing the growth of E. coli cultures. Our Lsp assay will be a useful tool for biologists to monitor Lsp activity and our inhibitors will facilitate development of antibacterial agents to potentially treat antibiotic-resistant bacteria.
• US5061800A
  申请人：——

  公开号：US5061800A

  公开（公告）日：1991-10-29
• Heinicke, Grant; Hung, Tran V.; Prager, Rolf H., Australian Journal of Chemistry, 1984, vol. 37, # 4, p. 831 - 844
  作者：Heinicke, Grant、Hung, Tran V.、Prager, Rolf H.、Ward, A. David

  DOI：——

  日期：——