快速的基基化学用于宏循环化
Ogonna Nwajiobi1, Ashish Kumar Verma1, Monika Raj1
1Department of Chemistry, Emory University, Atlanta, Georgia 30322, United States.
Journal of the American Chemical Society
|March 2, 2022
概括
我们开发了一种快速的化方法, 这产生稳定的循环,在紫外线或酸暴露时释放线性,从而使新的应用成为可能.
科学领域:
- 有机化学
- 化学生物学
- 类化学
背景情况:
- 对药物发现和化学生物学来说,的宏循环是至关重要的.
- 现有的方法通常需要保护群体或恶劣的条件.
- 开发快速和多样化的宏循环化策略是必不可少的.
研究的目的:
- 引入一种新的,快速的三策略,用于的宏循环.
- 制造具有刺激响应的三连接的循环.
- 证明该方法对各种结构和修改的适用性.
主要方法:
- 使用快速的三化学方法进行无保护的化学选择循环.
- 使用二次胺和p-氨基来形成三.
- 在紫外线辐射和酸性条件下研究响应刺激的环开放.
主要成果:
- 在一个中成功合成了18至66个单元单元和单元单元.
- 在中性pH和恶劣条件下证明了三循环的高稳定性.
- 展示刺激触发的完整线性的释放,然后再循环.
结论:
- 三策略提供了一种快速,高效和多用途的宏循环化方法.
- 由此产生的循环具有独特的刺激反应特性,可控制释放.
- 这种方法对药物输送,化学生物学和高通量查的应用具有前景.
相关概念视频
Thermal and Photochemical Electrocyclic Reactions: Overview
2.5K
Electrocyclic reactions are reversible reactions. They involve an intramolecular cyclization or ring-opening of a conjugated polyene. Shown below are two examples of electrocyclic reactions. In the first reaction, the formation of the cyclic product is favored. In contrast, in the second reaction, ring-opening is favored due to the high ring strain associated with cyclobutene formation.
2.5K
Radical Reactivity: Intramolecular vs Intermolecular
1.8K
Radical reactions can occur either intermolecularly or intramolecularly. In an intermolecular radical reaction, a nucleophilic radical adds to an electrophilic alkene or vice versa. In such reactions, the radical and generally the alkene, which is also called the radical trap, are two different molecules. Additionally, for such intermolecular reactions to occur, the radical trap must be active, present in an excess concentration, and the radical starting material must have a weak...
1.8K
Cycloaddition Reactions: Overview
2.9K
Cycloadditions are one of the most valuable and effective synthesis routes to form cyclic compounds. These are concerted pericyclic reactions between two unsaturated compounds resulting in a cyclic product with two new σ bonds formed at the expense of π bonds. The [4 + 2] cycloaddition, known as the Diels–Alder reaction, is the most common. The other example is a [2 + 2] cycloaddition.
2.9K
Cycloaddition Reactions: MO Requirements for Thermal Activation
3.8K
Thermal cycloadditions are reactions where the source of activation energy needed to initiate the reaction is provided in the form of heat. A typical example of a thermally-allowed cycloaddition is the Diels–Alder reaction, which is a [4 + 2] cycloaddition. In contrast, a [2 + 2] cycloaddition is thermally forbidden.
3.8K
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
3.1K
The reaction of weakly electrophilic aryldiazonium (also called arenediazonium) salts with highly activated aromatic compounds leads to the formation of products with an —N=N— link, called an azo linkage. This reaction, presented in Figure 1, is known as diazo coupling and occurs without the loss of the nitrogen atoms of the aryldiazonium salt. Highly activated aromatic compounds such as phenols or arylamines favor the diazo coupling reaction. The coupling generally occurs at the...
3.1K
Preparation of 1° Amines: Hofmann and Curtius Rearrangement Overview
3.3K
In the presence of an aqueous base and a halogen, primary amides can lose the carbonyl (as carbon dioxide) and undergo rearrangement to form primary amines. This reaction, called the Hofmann rearrangement, can produce primary amines (aryl and alkyl) in high yields without contamination by secondary and tertiary amines.
3.3K


![Solid-phase Synthesis of [4.4] Spirocyclic Oximes](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F58508.jpg&w=3840&q=50)