简洁和模块化基因酶总合成的双基素化物
Jin Wang1, Jianxiong Zhao2, Zhenyang Yu3
1Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, Beijing, 100871, People's Republic of China.
Angewandte Chemie (International ed. in English)
|September 21, 2024
概括
化学家们开发了高效的化学酶方法,在5-7个步骤中合成了8种双基素化物 (bisBIA). 这种方法使复杂的自然产品可用于生物研究的可扩展生产.
科学领域:
- 有机化学 有机化学
- 合成生物学 合成生物学
- 自然产品 化学 化学
背景情况:
- 双基素化物 (bisBIAs) 是一类具有显著生物活性的天然产品.
- 它们的复杂结构对传统合成方法构成挑战.
研究的目的:
- 开发一种融合和模块化化学酶策略,用于合成多种 bisBIA.
- 为了实现有效和可扩展的 bisBIAs enantiopure 的生产.
主要方法:
- 酶类立体选择性皮克特-斯勒反应用于单体合成.
- 用铜介导的乌尔曼合器用于线性bisBIA形成.
- 对宏环 bisBIAs 的生物模拟氧化二元化和分子内合.
主要成果:
- 在5-7个步骤中成功合成了8种不同的bisBIAs.
- 格拉姆尺度的生产的化化化素单体.
- 首次对三种宏环 bisBIA 进行了对抗选择性总合成.
结论:
- 化学酶策略为bisBIA合成提供了一种强大而通用的方法.
- 这项工作为进一步的生物研究提供了一系列bisBIA.
相关概念视频
Preparation of 1° Amines: Gabriel Synthesis
3.5K
Direct alkylation is not a suitable method for synthesizing amines because it produces polyalkylated products. Gabriel synthesis is the most preferred method to exclusively make primary amines. The method uses phthalimide, which contains a protected form of nitrogen that participates in alkylation only once to predominantly give primary amines.
Strong bases like NaOH or KOH deprotonate the phthalimide to form the corresponding anion, which acts as a nucleophile. Further, the anion attacks an...
Strong bases like NaOH or KOH deprotonate the phthalimide to form the corresponding anion, which acts as a nucleophile. Further, the anion attacks an...
3.5K
Prochirality
3.8K
The concept of prochirality leads to the nomenclature of the individual faces of a molecule and plays a crucial role in the enantioselective reaction. It is a concept where two or more achiral molecules react to produce chiral products. A typical process is the reaction of an achiral ketone to generate a chiral alcohol. Here, the achiral reactant reacts with an achiral reducing agent, sodium borohydride, to generate an equimolar mixture of the chiral enantiomers of the product. For example, an...
3.8K
Nucleophilic Aromatic Substitution: Elimination–Addition
4.0K
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...
4.0K


![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)