Regiocontrolled palladium-catalyzed direct C2-arylation of a difluorobenzo[d]imidazole
作者： Thierry Roisnel , Henri Doucet , Hai-Yun Huang , Haoran Li
DOI: 10.1016/J.TETLET.2021.153112
关键词: Medicinal chemistry 、 Regioselectivity 、 Ring (chemistry) 、 Chemistry 、 Bromide 、 Palladium 、 Imidazole 、 Catalysis 、 Site selectivity 、 Aryl
摘要: Abstract Conditions for the regioselective palladium-catalyzed direct arylation of a 6,7-difluorobenzo[d]imidazole using aryl bromides as coupling partners are described. The site selectivity was found to be in favor C2-carbon difluorobenzo[d]imidazole; whereas difluoro-substituted ring remained untouched, even presence an excess bromide. This method tolerates variety substituents at para-, meta- and ortho-positions on bromide also N-containing heteroaryl bromides.
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