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Palladium-Catalyzed Direct C7-Arylation of Substituted Indazoles
A novel direct C7-arylation
of indazoles with iodoaryls is described
using PdĀ(OAc)<sub>2</sub> as catalyst, 1,10-phenanthroline as ligand,
and K<sub>2</sub>CO<sub>3</sub> as base in refluxing DMA. Direct C7-arylation
of 3-substituted 1<i>H</i>-indazole containing an EWG on
the arene ring gave the expected products in good isolated yields.
In addition, a one-pot SuzukiāMiyaura/arylation procedure leading
to C3,C7-diarylated indazoles has been developed