摘要/Abstract
苯酚及其衍生物既广泛地存在于自然界中又是药物分子的重要骨架.同时,苯酚衍生物还是非常重要的有机合成中间体.近几年,随着过渡金属催化C-H键活化的发展,通过C-H键的切断实现直接羟基化制备苯酚衍生物的方法被越来越多的有机化学家所关注.综述了最近对芳香环C-H键羟基化制备苯酚衍生物方法的研究进展,通过不同羟基源的使用对该类型的反应进行分类讨论,对底物适应范围和反应机理等进行了详细论述,并就该领域的局限性和未来的发展前景进行总结和展望.
关键词: 过渡金属催化, 碳氢活化, 羟基化, 苯酚
Phenols are important central motifs that are abundant in many natural products, pharmaceuticals and agrochemicals. Moreover, the high reactivity of phenol derivatives makes them versatile building blocks for organic synthesis. Over the past decade, the synthesis of phenol derivatives via C-H hydroxylation of aromatics has received much attention due to its potential as an atom efficient methodology. Herein, the research advances on the C-H hydroxylation of aromatics are reviewed categorized by the types of hydroxylation source used. Detailed substrate scopes and reaction mechanisms will be discussed, as well as the limitations of current procedures and the prospects for the future.
Key words: transition-metal catalysis, C-H activation, hydroxylation, phenols
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