Palladium-Catalyzed intramolecular direct arylation of aromatic tertiary amide compounds revisited
Palladium-Catalyzed intramolecular direct arylation of aromatic tertiary amide compounds revisited
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钯催化芳香族叔酰胺化合物分子内直接芳基化反应的再探讨
DOI：
10.1016/j.rechem.2022.100432
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发表时间：
2022
影响因子：
2.3
通讯作者：
Tsunekawa Ryotaro
中科院分区：
文献类型：
--
作者：
Takagi Koji;Maeda Asuka;Tsunekawa Ryotaro
研究了钯催化的三种芳香叔酰胺化合物的分子内直接芳基化反应。对于苯环的C-H活化，在PCy 3·HBF 4和PivOH存在下加热超过120 °C是必需的，并且不能抑制区域异构体的形成。支链烷基链的引入阻碍了反应的顺利进行。相反，吡啶环的C-H活化甚至在100 °C下进行，并且定量地获得目标化合物。这些结果得到了理论DFT计算的定性支持。
We have investigated the palladium-catalyzed intramolecular direct arylation of three aromatic tertiary amide compounds. For the C–H activation of the benzene ring, heating over 120 °C in the presence of PCy3·HBF4and PivOH was indispensable, and the formation of the regioisomer could not be suppressed. The introduction of a branched alkyl chain hampered the smooth reaction. In contrast, the C–H activation of the pyridine ring proceeded even at 100 °C, and the target compound was obtained quantitatively. These results were qualitatively supported by theoretical DFT calculations.