奇拉BCPs的enantioselective合成 奇拉BCPs的enantioselective合成 奇拉BCPs的enantioselective合成 奇拉BCPs的选择性合成
Irene Sánchez-Sordo1, Sergio Barbeira-Arán1, Martín Fañanás-Mastral1
1Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CiQUS), Universidade de Santiago de Compostela 15782 Santiago de Compostela Spain martin.fananas@usc.es.
自行车[1.1.1] (BCP) 是一种有价值的药物设计支架. 本综述涵盖了性BCP的不对称合成方法,增强药物特性和扩大化学空间.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 药物设计 药物设计
背景情况:
- 自行车[1.1.1]坦 (BCP) 是紧张的循环支架,在药物发现方面具有重大潜力.
- BCPs作为环,三基和基的有效生物异构体,改善候选药物的药理动力学和物理化学特性.
研究的目的:
- 审查和讨论现有的催化方法对阿尔法 - 奇拉双循环[1.1.1]pentanes.pentanes的不对称合成.
- 突出这些不对称转换的机制方面.
- 为了探索在药物设计中的生物异构体替代品中性BCP的应用.
主要方法:
- 对BCP的催化不对称合成策略的讨论.
- 分析所讨论的转换的关键机械特征.
- 在药物化学和药物开发中审查BCP应用.
主要成果:
- 对各种不对称的合成路线的概述,以访问合性BCP.
- 确定BCP作为新药类型的多功能构建块.
- 通过结合BCP来证明改善药物特性.
结论:
- 不对称的BCP合成对于扩大其在药物设计中的实用性至关重要.
- 石化BCP为药用化学提供独特的结构和电子特性.
- 进一步开发催化方法将加速BCP在药品中的应用.
更多相关视频
10:17Efficient Construction of Drug-like Bispirocyclic Scaffolds Via Organocatalytic Cycloadditions of α-Imino γ-Lactones and Alkylidene Pyrazolones
Published on: February 7, 2019
11:09Constructing Thioether/Vinyl Sulfide-tethered Helical Peptides Via Photo-induced Thiol-ene/yne Hydrothiolation
Published on: August 1, 2018
相关概念视频
Prochirality
Chirality in Nature
Diels–Alder Reaction Forming Bridged Bicyclic Products: Stereochemistry
Chirality at Nitrogen, Phosphorus, and Sulfur
A consequence of chirality is the need for enantiomeric resolution. While this is theoretically possible for all...
Preparation of 1° Amines: Azide Synthesis
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...
SN1 Reaction: Stereochemistry
In the first step of an SN1 reaction, the bond between the electrophilic carbon and the leaving group ionizes to generate the carbocation intermediate. The second step of the mechanism is the nucleophilic attack.
In the formed carbocation, the positively charged carbon is sp2 hybridized with a trigonal planar geometry. As all the three substituents lie on the same plane, a plane of symmetry for the...
