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钯催化的二氟甲基芳基化的研究进展
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Abstract:
增加生物活性分子的亲脂性、代谢稳定性、药代动力学特征的有效方法之一是在其分子结构中引入含氟基团，特别是二氟甲基。在过去的十年中，基于过渡金属催化完成二氟甲基芳基化的方法已经被证明是有效的策略。这些方法主要包括两类：一是芳烃的预官能团化，二是开发各类二氟甲基化试剂，其中由钯催化的二氟甲基芳基化的反应表现出优异的选择性、广泛的官能团耐受性、温和的反应条件等众多优点。鉴于二氟甲基在各个领域的重要性，本文主要总结了钯催化的二氟甲基芳基化的反应研究进展，反应涵盖至2024年。
One of the effective methods to enhance the lipophilicity, metabolic stability, and pharmacokinetic properties of bioactive molecules is to introduce fluorine-containing groups, especially difluoromethyl groups, into their molecular structures. Over the past decade, transition metal-catalyzed methods for difluoromethyl arylation have been proven to be an effective strategy. These methods mainly fall into two categories: pre-functionalization of aromatic compounds and development of various difluoromethylating reagents. Among them, palladium-catalyzed difluoromethyl arylation reactions exhibit numerous advantages, such as excellent selectivity, broad functional group tolerance, and mild reaction conditions. Given the significance of difluoromethyl groups in various fields, this review mainly summarizes the research progress of palladium-catalyzed difluoromethyl arylation reactions, covering studies up to 2024.
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