Direct C3-Arylation of 2H-Indazole Derivatives with Aryl Bromides by using Low Loading of a Phosphine-free Palladium Catalyst

Abstract : The palladium-catalyzed direct arylation of 2 H-indazoles with aryl bromides for the preparation of 3-aryl-2 H-indazoles was found to proceed in high yields when using only 0.5–0.1 mol % Pd(OAc)2 catalyst and KOAc as inexpensive base. A wide variety of electron-deficient and electron-rich aryl bromides and also heteroaryl bromides has been successfully employed. Both electron-withdrawing and electron-donating substituents on the 2 H-indazoles are also tolerated. Moreover, the reaction can be performed in the “green” solvent cyclopentyl methyl ether.
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Fatma Belkessam, Mohand Aidene, Jean-François Soulé, Henri Doucet. Direct C3-Arylation of 2H-Indazole Derivatives with Aryl Bromides by using Low Loading of a Phosphine-free Palladium Catalyst. ChemCatChem, Wiley, 2017, 9 (12), pp.2239--2249. ⟨10.1002/cctc.201601420⟩. ⟨hal-01578529⟩

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