实际的二环醇代谢物M2和M3的グラム级合成
Bo Ma1, Zhen-Wei Wang1, Xiao-Yu Liu1
1State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Journal of Asian natural products research
|November 7, 2023
概括
研究人员开发了一种新合成的bicyclol代谢物M2和M3. 这种高效的方法提供了足够的数量来研究药物相互作用,并确保用于乙型肝炎的药物bicyclol的安全性和有效性.
科学领域:
- 药用化学 医学化学
- 有机合成 有机合成
- 药理学 药理学是指药理学的学科.
背景情况:
- 比西克罗尔是一种肝脏保护药物,在中国批准用于乙型肝炎和药物诱导的肝损伤.
- 活性代谢物M2和M3对于了解bicyclol的药物相互作用至关重要.
- 需要足够的M2和M3量来评估它们对药物安全性和有效性的影响.
研究的目的:
- 开发一种新的,高效的合成路径,用于bicyclol代谢物M2和M3.
- 为了进一步进行药理学研究,使M2和M3能够在克尺度上进行合成.
- 促进评估涉及M2和M3的潜在药物相互作用.
主要方法:
- 作为关键的合成步骤,苏子基-宫拉合反应是关键的合成步骤.
- 开发一种简洁而新的合成途径.
- 针对可扩展性的反应条件的优化.
主要成果:
- 成功合成了M2和M3的新路线.
- 达到两种代谢产物的克尺度数量.
- 建立了生产M2和M3的可靠方法.
结论:
- 开发的合成途径对生产M2和M3具有高效性.
- 格拉姆级合成使得全面的DDI研究成为可能.
- 这项工作支持对双醇治疗的安全性和疗效的评估.
相关概念视频
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
Preparation of 1° Amines: Gabriel Synthesis
3.6K
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...
3.6K
Cycloaddition Reactions: Overview
2.6K
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.
2.6K
Alkylation of β-Diester Enolates: Malonic Ester Synthesis
3.4K
Malonic ester synthesis is a method to obtain α substituted carboxylic acids from ꞵ-diesters such as diethyl malonate and alkyl halides.
3.4K


