相关实验视频
Updated: Sep 19, 2025

07:11
Constructing Cyclic Peptides Using an On-Tether Sulfonium Center
Published on: September 28, 2022
2.8K
循环的合成使用烯-氨基醇点击化学
Sven Ullrich1, Christoph Nitsche2
1Research School of Chemistry, Australian National University, Canberra, ACT, Australia.
Methods in molecular biology (Clifton, N.J.)
|June 18, 2025
概括
我们开发了一种生物相容的方法,用于使用非正规氨基酸合成循环. 这种可访问的协议可以在水溶液中有效地形成双循环,用于治疗开发.
科学领域:
- 药用化学 医学化学
- 生物技术是生物技术.
- 合成生物学 合成生物学
背景情况:
- 约束在药物发现中是有价值的,因为它们的稳定性和特定的形状.
- 已经确立了循环和接的生物相容方法,但双循环生成仍未得到充分探索.
- 体自行车为治疗应用提供独特的结构性质.
研究的目的:
- 开发一种生物相容且易于使用的合成循环的方法.
- 解决对有效和选择性生成双循环的需求.
- 提供使用非正规氨基酸进行类循环合成的详细协议.
主要方法:
- 结合非正规氨基酸的线性前体的固相合成.
- 利用κυανοπυριδίνη和1,2-aminothiol的活性进行循环.
- 从商业上可用的构建模块中合成非正规氨基酸的树脂合成.
主要成果:
- 成功合成能够形成双循环结构的前体.
- 在生理pH的水性缓冲物中有效循环.
- 该协议可用于有限的合成化学资源的实验室.
结论:
- 已经建立了一个新的,生物相容的策略,用于类自行车合成.
- 开发的方法有助于生成受约束,用于治疗开发.
- 该协议简化了复杂结构的合成.
相关概念视频
Preparation of 1° Amines: Azide Synthesis
4.1K
Direct alkylation of ammonia produces polyalkylated amines, along with a quaternary ammonium salt. To exclusively prepare primary amines, the azide synthesis method can be used.
Azide ions act as good nucleophiles and react with unhindered alkyl halides to form alkyl azides. Alkyl azides do not participate in further nucleophilic substitution reactions, thereby eliminating the chances of polyalkylated products. Alkyl azides are reduced by hydride-based reducing agents, like lithium aluminum...
Azide ions act as good nucleophiles and react with unhindered alkyl halides to form alkyl azides. Alkyl azides do not participate in further nucleophilic substitution reactions, thereby eliminating the chances of polyalkylated products. Alkyl azides are reduced by hydride-based reducing agents, like lithium aluminum...
4.1K
Preparation of Amides
3.3K
Amides are synthesized by treating carboxylic acids with amines in the presence of dehydrating agents like dicyclohexylcarbodiimide (DCC).
The DCC-promoted synthesis of amides begins with the protonation of DCC by carboxylic acid. The protonation makes it a better acceptor. Next, the addition of carboxylate to the protonated carbodiimide gives a reactive acylating agent.
Subsequently, the amine acts as a nucleophile that attacks the acylating agent to form a tetrahedral intermediate. In the...
The DCC-promoted synthesis of amides begins with the protonation of DCC by carboxylic acid. The protonation makes it a better acceptor. Next, the addition of carboxylate to the protonated carbodiimide gives a reactive acylating agent.
Subsequently, the amine acts as a nucleophile that attacks the acylating agent to form a tetrahedral intermediate. In the...
3.3K
Preparation of 1° Amines: Gabriel Synthesis
3.8K
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...
3.8K
Cycloaddition Reactions: Overview
2.8K
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.
2.8K
Peptide Bonds
77.5K
A peptide bond covalently attaches amino acids through a dehydration reaction. One amino acid's carboxyl group and another amino acid's amino group combine, releasing a water molecule. The resulting bond is the peptide bond. The products that such linkages form are peptides. As more amino acids join this growing chain, the resulting chain is a polypeptide. Each polypeptide has a free amino group at one end. This end has the N-terminal, or the amino-terminal, and the other end has a free...
77.5K

