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相关概念视频

Phase II Reactions: Methylation Reactions01:17

Phase II Reactions: Methylation Reactions

611
Methylation is a phase II biotransformation process involving the attachment of a methyl group to a substrate. Enzymes known as methyltransferases orchestrate this reaction.
The mechanism of methylation unfolds in two stages. The first stage sees a methyltransferase enzyme facilitating the transfer of a methyl group from S-adenosylmethionine (SAM) to the substrate, forming S-adenosylhomocysteine (SAH). The second stage involves further metabolism of SAH into homocysteine, which can be recycled...
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Oxidation of Alkenes: Anti Dihydroxylation with Peroxy Acids02:04

Oxidation of Alkenes: Anti Dihydroxylation with Peroxy Acids

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Diols are compounds with two hydroxyl groups. In addition to syn dihydroxylation, diols can also be synthesized through the process of anti dihydroxylation. The process involves treating an alkene with a peroxycarboxylic acid to form an epoxide. Epoxides are highly strained three-membered rings with oxygen and two carbons occupying the corners of an equilateral triangle. This step is followed by ring-opening of the epoxide in the presence of an aqueous acid to give a trans diol.
7.1K
Oxidation of Alcohols02:37

Oxidation of Alcohols

15.4K
In this lesson, the oxidation of alcohols is discussed in depth. The various reagents used for oxidation of primary and secondary alcohols are detailed, and their mechanism of action is provided.
The process of oxidation in a chemical reaction is observed in any of the three forms:
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Oxidation of Alkenes: Syn Dihydroxylation with Osmium Tetraoxide02:44

Oxidation of Alkenes: Syn Dihydroxylation with Osmium Tetraoxide

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Alkenes are converted to 1,2-diols or glycols through a process called dihydroxylation. It involves the addition of two hydroxyl groups across the double bond with two different stereochemical approaches, namely anti and syn. Dihydroxylation using osmium tetroxide progresses with syn stereochemistry.
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Phase I Reactions: Oxidation of Carbon-Heteroatom and Miscellaneous Systems01:15

Phase I Reactions: Oxidation of Carbon-Heteroatom and Miscellaneous Systems

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Oxidative reactions are pivotal in metabolizing numerous compounds, including pharmaceutical drugs. These reactions often occur in carbon-heteroatom systems, such as carbon-nitrogen, carbon-sulfur, and carbon-oxygen.
In carbon-nitrogen systems, aliphatic and aromatic amines can undergo oxidative reactions. Secondary and tertiary amines, like those found in tricyclic antidepressants, can undergo N-dealkylation, a process that involves the oxidation of the alkyl group. In addition, oxidative...
340
Phase II Reactions: Acetylation Reactions01:24

Phase II Reactions: Acetylation Reactions

661
Acetylation, a phase II biotransformation reaction, introduces an acetyl group to drugs or their metabolites. Acetyltransferase enzymes facilitate this reaction, which resembles α-amino acid conjugation due to the addition of a functional group to the drug molecule.
The substrates for acetylation are typically drugs or their metabolites with an amino, sulfonamide, or hydrazine functional group. Acetylation can occur at several points in the drug molecule, including primary, secondary, and...
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最后阶段的氧化C-H甲基化

Kaibo Feng1, Raundi E Quevedo1, Jeffrey T Kohrt2

  • 1Department of Chemistry, Roger Adams Laboratory, University of Illinois, Urbana, IL, USA.

Nature
|March 18, 2020
PubMed
概括

这项研究引入了一种新方法,用于将甲基组添加到复杂分子中,从而提高药物的效力. 这种晚期C(sp3) -H甲基化技术是高效的,在药物化学中广泛适用.

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科学领域:

  • 有机化学 有机化学
  • 药用化学 医学化学
  • 催化剂是一种催化剂.

背景情况:

  • "神奇的甲基效应"通过添加甲基组,特别是与异构原子相邻的甲基组,显著提高了生物活性分子的效力.
  • 现有的甲基化方法在复杂分子结构的范围和适用性方面存在局限性,阻碍了药物开发.

研究的目的:

  • 开发一种区域选择性和化学选择性氧化C(sp3) -H甲基化方法,用于药物支架和天然产品的后期功能化.
  • 为了使复杂分子的有效和有针对性的甲基化,促进"神奇的甲基效应"的探索.

主要方法:

  • 一种新的方法,结合了选择性C-H氧化与使用催化剂 (Mn(CF3PDP)) 的温和,功能组耐受性甲基化.
  • 使用或易斯酸辅助的活性中间体形成,用于用有机试剂进行甲基化.
  • 将该方法应用于41种不同的基质,包括医学上重要的核心,药物和自然产品.

主要成果:

  • 在18种药理学上相关的分子上实现了选择性C ((sp3) -H末期甲基化,包括Tedizolid和天然产品等药物.
  • 通过晚期甲基化证明了两种"神奇甲基"候选药物的成功合成.
  • 在abiraterone类似物上展示了远程甲基化,强调了该方法的多功能性.

结论:

  • 开发的方法为晚期C(sp3) -H甲基化提供了一个强大的工具,与复杂的药物架构和天然产品兼容.
  • 这种技术显著减少了合成的努力,加速了新疗法和化学探针的发现和开发.
  • 扩大了"神奇甲基效应"在药物化学研究中的应用.