Palladium-Catalyzed Direct C7-Arylation of Substituted Indazoles
2014
Naas, Mohammed | El Kazzouli, Saı̈d | Essassi, El Mokhtar | Bousmina, Mosto | Guillaumet, Gérald
A novel direct C7-arylation of indazoles with iodoaryls is described using Pd(OAc)₂ as catalyst, 1,10-phenanthroline as ligand, and K₂CO₃ as base in refluxing DMA. Direct C7-arylation of 3-substituted 1H-indazole containing an EWG on the arene ring gave the expected products in good isolated yields. In addition, a one-pot Suzuki–Miyaura/arylation procedure leading to C3,C7-diarylated indazoles has been developed.
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