吡唑定向、不含氟醇的 C-H 键芳基化反应

Le Van Lam, Nguyen Thanh Tung
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引用次数: 0

摘要

sp2 C-H 键的定向芳基化通常被认为是快速提高有机分子复杂性的最便捷方法之一。然而,现有的大多数方法都使用六氟异丙醇(HFIP)等氟醇作为溶剂。在此,我们报告了一种使用乙酸溶剂,在钯催化下对炔烃 C-H 键进行定向芳基化的简单方法。成功的官能化依赖于吡唑定向基团的使用。
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Pyrazole-directed, fluoroalcohol-free arylation of C-H bonds
Directed arylation of sp2 C−H bonds is often considered one of the most convenient methods to rapidly increase the complexity of organic molecules. However, most of the available methods utilized fluoroalcohols such as hexafluoroisopropanol (HFIP) as the solvent. Herein we report a simple method for palladium-catalyzed, directed arylation of arene C−H bond using acetic acid solvent. The successful functionalization relies on the use of pyrazole directing group.
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