(S)-1-((tert-butyldiphenylsilyl)oxy)butan-2-amine | 429669-41-0

• 分子结构分类: 有机化合物 - 有机金属化合物 - 有机类金属化合物
• 英文名称: (S)-1-((tert-butyldiphenylsilyl)oxy)butan-2-amine
• 英文别名: (1S)-1-(t-butyldiphenylsilyloxymethyl)propylamine；(2S)-1-[tert-butyl(diphenyl)silyl]oxybutan-2-amine
• CAS: 429669-41-0
• 化学式: C₂₀H₂₉NOSi
• 分子量: 327.542
• InChiKey: LFJHBORSSMUGOR-KRWDZBQOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  23
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  35.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (S)-1-((tert-butyldiphenylsilyl)oxy)butan-2-amine 、 氯乙酰氯 在 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 16.0h， 以51%的产率得到(S)-N-(1-((tert-butyldiphenylsilyl)oxy)butan-2-yl)-2-chloroacetamide
  参考文献：
  名称：

  Design, synthesis, and evaluation of novel ethambutol analogues

  摘要：

  Ethambutol is one of the front-line agents recommended by the World Health Organization for the treatment of tuberculosis. In an effort to develop more potent therapies to treat tuberculosis, novel unsymmetrical ethambutol analogues were successfully synthesized by a new route utilizing novel building blocks synthesized using Ellman's sulfinyl chemistry. The resulting analogues were tested for anti-tuberculosis activity yielding compounds with comparable anti-tuberculosis activity to ethambutol and increased lipophilicity that may instill better tissue penetration and serum half-life. (c) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.01.065
• 作为产物：
  描述：

  [(1S)-1-(t-butyldiphenylsilyloxymethyl)propyl]carbamic acid benzyl ester 在 钯 silica gel 作用下， 以 甲醇 为溶剂， 反应 4.0h， 以to afford (1S)-1-(t-butyldiphenylsilyloxymethyl)propylamine (2.32 g, yield 88%) as a colorless oil的产率得到(S)-1-((tert-butyldiphenylsilyl)oxy)butan-2-amine
  参考文献：
  名称：

  1-methylcarbapenem derivatives

  摘要：

  本发明涉及一种由式（I）表示的1-甲基碳青霉烯化合物，具有抗菌活性，其药理学上可接受的酯类或盐类，以及含有它们作为活性成分的制药组合物（特别是抗菌剂）。此外，本发明还包括使用这些化合物、酯衍生物或盐类制备制药组合物的方法，或通过向温血动物（特别是人类）施用药理学有效量的这些化合物、酯衍生物或盐类来预防或治疗疾病（特别是细菌感染）。

  公开号：

  US07001897B2

文献信息

• 1-Methylcarbapenem derivatives
  申请人：SANKYO COMPANY, LIMITED

  公开号：US20040014962A1

  公开（公告）日：2004-01-22

  1-Methylcarbapenem compounds having antibacterial activity, pharmacologically acceptable esters or salts thereof and pharmaceutical compositions (particularly antibacterial agents) containing them as an active ingredient are described. In addition, the invention includes the use of these compounds, ester derivatives or salts for the manufacture of pharmaceutical compositions, or a method for the prevention or treatment of diseases (particularly bacterial infections) by administering a pharmacologically effective amount of the compounds, ester derivatives or salts to warm-blooded animals (particularly human beings).

  描述了具有抗菌活性的1-甲基碳青霉烯化合物、它们的药物可接受的酯或盐，以及含有它们作为活性成分的药物组合物（特别是抗菌剂）。此外，发明包括这些化合物、酯衍生物或盐用于制造药物组合物，或通过向温血动物（特别是人类）投给药物有效量的这些化合物、酯衍生物或盐，用于预防或治疗疾病（特别是细菌感染）的方法。
• Ligand-Enabled Palladium(II)-Catalyzed γ-C(sp³)–H Arylation of Primary Aliphatic Amines
  作者：Chen-Hui Yuan、Lei Jiao

  DOI：10.1021/acs.orglett.3c03186

  日期：2024.1.12

  The Pd(II)/sulfoxide-2-hydroxypyridine catalytic system shows promising activity in C–H activation chemistry. In this study, we showcase how this catalytic system solves the problem of native primary amine-directed γ-C(sp3)–H arylation. Primary amines with different complexities are compatible with the established methodology, and the range of applicable substrates can be expanded to include pyridine

  Pd(II)/亚砜-2-羟基吡啶催化体系在 C-H 活化化学中表现出良好的活性。在这项研究中，我们展示了该催化系统如何解决天然伯胺导向的 γ-C(sp 3 )–H 芳基化问题。不同复杂度的伯胺与已建立的方法兼容，并且适用的底物范围可以扩大到包括吡啶、肟醚和吡啶N-氧化物。
• Design, synthesis, and evaluation of novel ethambutol analogues
  作者：Raghunandan Yendapally、Richard E. Lee

  DOI：10.1016/j.bmcl.2008.01.065

  日期：2008.3

  Ethambutol is one of the front-line agents recommended by the World Health Organization for the treatment of tuberculosis. In an effort to develop more potent therapies to treat tuberculosis, novel unsymmetrical ethambutol analogues were successfully synthesized by a new route utilizing novel building blocks synthesized using Ellman's sulfinyl chemistry. The resulting analogues were tested for anti-tuberculosis activity yielding compounds with comparable anti-tuberculosis activity to ethambutol and increased lipophilicity that may instill better tissue penetration and serum half-life. (c) 2008 Elsevier Ltd. All rights reserved.
• 1-methylcarbapenem derivatives
  申请人：Sankyo Company, Limited

  公开号：US07001897B2

  公开（公告）日：2006-02-21

  A 1-methylcarbapenem compound represented by the formula (I): having antibacterial activity, pharmacologically acceptable esters or salts thereof and pharmaceutical compositions (particularly antibacterial agents) containing them as an active ingredient are described. In addition, the invention includes the use of these compounds, ester derivatives or salts for the manufacture of pharmaceutical compositions, or a method for the prevention or treatment of diseases (particularly bacterial infections) by administering a pharmacologically effective amount of the compounds, ester derivatives or salts to warm-blooded animals (particularly human beings).

  本发明涉及一种由式（I）表示的1-甲基碳青霉烯化合物，具有抗菌活性，其药理学上可接受的酯类或盐类，以及含有它们作为活性成分的制药组合物（特别是抗菌剂）。此外，本发明还包括使用这些化合物、酯衍生物或盐类制备制药组合物的方法，或通过向温血动物（特别是人类）施用药理学有效量的这些化合物、酯衍生物或盐类来预防或治疗疾病（特别是细菌感染）。