多组分反应 (MCRs) 产生医学相关的环:最近的更新和化学空间分析的支架
Mukesh Tandi1, Vaibhav Sharma1, Balasubramanian Gopal2
1Department of Pharmacy, Birla Institute of Technology and Science Pilani Pilani Campus Rajasthan 333031 India sandeep.sundriyal@pilani.bits-pilani.ac.in.
RSC advances
|January 17, 2025
概括
本综述强调了最近的多元组分反应 (MCR) 用于创建循环结构,重点关注那些具有药物化学应用的反应. 这些高效的单反应从简单的原料中产生新型化合物.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 合成化学 合成化学
背景情况:
- 多元组分反应 (MCR) 是有效合成复杂分子的强大工具.
- 最近的进展扩大了MCRs用于生成循环结构的范围.
- 专注于与药物化学相关的MCR对于药物发现至关重要.
研究的目的:
- 审查自2019年以来用于循环结构合成的最近的多组分反应 (MCR).
- 突出在药物化学中具有重大潜力的MCR.
- 描述由这些MCRs产生的支架的化学空间.
主要方法:
- 自2019年以来出版的MCRs的文献综述.
- 专注于在温和条件下的单反应.
- 合成方案,基质范围,区域和立体选择性的分析.
- 获得的脚手架的化学信息分析.
主要成果:
- 汇编了产生具有药物化学相关性的循环结构的MCR.
- 使用易于获得的构建块和温和条件识别反应.
- 与现有药物相比,MCR支架的特征是新的,复杂的和球状的.
结论:
- MCRs为药物发现提供了对新型循环支架的高效访问.
- 最近的MCR提供了多样化和复杂的分子架构.
- 本次审查有助于通过MCR探索和利用新的化学空间.
相关概念视频
Diels–Alder Reaction Forming Cyclic Products: Stereochemistry
3.7K
The Diels–Alder reaction is one of the robust methods for synthesizing unsaturated six-membered rings. The reaction involves a concerted cyclic movement of six π electrons: four π electrons from the diene and two π electrons from the dienophile.
3.7K
Diels–Alder Reaction Forming Bridged Bicyclic Products: Stereochemistry
4.6K
Diels–Alder reactions between cyclic dienes locked in an s-cis configuration and dienophiles yield bridged bicyclic products.
4.6K
Cycloaddition Reactions: Overview
2.5K
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.
2.5K
Olefin Metathesis Polymerization: Ring-Opening Metathesis Polymerization (ROMP)
2.5K
Ring-opening metathesis polymerization or ROMP involves strained cycloalkenes as starting materials. The mechanism of ROMP proceeds by reacting cycloalkene with Grubbs catalyst to give metallacyclobutane intermediate which undergoes a ring-opening reaction to form new carbene. The new carbene reacts with another molecule of cycloalkene. Repetition of these steps leads to the formation of an unsaturated open-chain polymer product. All these steps are reversible, however, relieving the ring...
2.5K
Stereoisomerism of Cyclic Compounds
8.7K
In this lesson, we delve into the role of ring conformation and its stability, which determines the spatial arrangement and, consequently, the molecular symmetry and stereoisomerism of cyclic compounds. 1,2-Dimethylcyclohexane is used as a case study to evaluate the possible number of stereoisomers. Here, given the multiple (n = 2) chiral centers, there are 2n = 4 possible configurations that lack a plane of symmetry, as the ring skeleton exists in a non-planar chair conformation. In addition,...
8.7K
[4+2] Cycloaddition of Conjugated Dienes: Diels–Alder Reaction
10.0K
The Diels–Alder reaction is an example of a thermal pericyclic reaction between a conjugated diene and an alkene or alkyne, commonly referred to as a dienophile. The reaction involves a concerted movement of six π electrons, four from the diene and two from the dienophile, forming an unsaturated six-membered ring. As a result, these reactions are classified as [4+2] cycloadditions.
10.0K


![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)