相关实验视频
Updated: Jan 14, 2026

11:51
Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
12.3K
通过单原子碳插入删除进行骨编辑
Di Tian1, Lu-Sen Yang1, Peng Yuan1
1Shanghai Frontiers Science Center for Drug Target Identification and Delivery, Laboratory of Innovative Immunotherapy, and Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, School of Pharmaceutical Sciences, Shanghai Jiao Tong University, Shanghai 200240, China.
Journal of the American Chemical Society
|October 21, 2025
概括
研究人员开发了一种直接将芳香碳转化为阿扎伦的新方法. 这种单碳插入和删除技术使得特定地点的骨重建成为可能,有助于药物发现.
科学领域:
- 有机化学
- 合成化学
- 医学化学
背景情况:
- 调整分子的特定功能往往取决于微小的原子变化.
- 在芳香系统中直接的碳转化具有挑战性,通常需要并行合成等间接方法.
研究的目的:
- 报告一种用于直接将芳香碳转化为阿扎伦的新型转化.
- 通过单碳插入和删除,使阿萨雷因支架的特定位置编辑成为可能.
主要方法:
- 用缺电子的基对阿萨雷因进行循环重组.
- 形成一个可异构的三烯的benzepine中间体.
- 区域选择性6π-aza电循环和碳离开
主要成果:
- 将两个相邻的芳香碳直接转化为新的碳,重建素.
- 通过同时进行1,2-碳迁移和插入新的可功能化碳来实现骨重建.
- 展示了广泛的基质范围,包括醇和相关的阿扎伦.
结论:
- 开发的方法避免了环开放和回收用于阿萨林修饰.
- 这种转化促进了药物分子的后期修饰.
- 通过单碳操纵能够精确地编辑阿扎伦的骨.
相关概念视频
RNA Editing
9.8K
RNA editing is a post-transcriptional modification where a precursor mRNA (pre-mRNA) nucleotide sequence is changed by base insertion, deletion, or modification. The extent of RNA editing varies from a few hundred bases, in mitochondrial DNA of trypanosomes, to a just single base, in nuclear genes of mammals. Even a single base change in the pre-mRNA can convert a codon for one amino acid into the codon for another amino acid or a stop codon. This type of re-coding can significantly affect the...
9.8K
Oxidation of Phenols to Quinones
4.5K
In the presence of oxidizing agents, phenols are oxidized to quinones. Quinones can be easily reduced back to phenols using mild reducing agents. The electron-donating hydroxyl group enhances the reactivity of the aromatic ring, enabling oxidation of the ring even in the absence of an α hydrogen.
o-hydroxy phenols are oxidized to o-quinones and p-hydroxy phenols to p-quinones. Such redox reactions involve the transfer of two electrons and two protons. The reversible redox...
o-hydroxy phenols are oxidized to o-quinones and p-hydroxy phenols to p-quinones. Such redox reactions involve the transfer of two electrons and two protons. The reversible redox...
4.5K
Carbon Skeletons
113.9K
Life on Earth is carbon-based, as all macromolecules that make up living organisms contain carbon atoms. All organic compounds have a carbon backbone. Each carbon atom is tetravalent and can bond with four other atoms, making it an extraordinarily flexible component of biological molecules. Because carbon’s valence electrons are stable, it rarely becomes an ion. As the carbon chain increases in length, structural modifications such as ring structures, double bonds, and branching side...
113.9K
Nucleophilic Aromatic Substitution: Elimination–Addition
5.0K
Simple aryl halides do not react with nucleophiles. However, nucleophilic aromatic substitutions can be forced under certain conditions, such as high temperatures or strong bases. The mechanism of substitution under such conditions involves the highly unstable and reactive benzyne intermediate. Benzyne contains equivalent carbon centers at both ends of the triple bond, each of which is equally susceptible to nucleophilic attack. This 50–50 distribution of products is...
5.0K
Radical Chain-Growth Polymerization: Overview
3.1K
Chain-growth or addition polymerization is successive addition reactions of monomers with a polymer chain. In radical chain-growth polymerization, the reaction proceeds via a free-radical intermediate. The free radical is formed from radical initiators, which spontaneously generate free radicals by homolytic fission. Organic peroxides (such as dibenzoyl peroxide, as shown in Figure 1) or azo compounds are popular radical initiators. A low concentration ratio of radical initiator to monomer is...
3.1K
Nucleotide Excision Repair
40.6K
Overview
40.6K

