Palladium‐Catalyzed Regioselective C−H Arylation of 4‐Azaindazole at C3, C5 and C7 Positions - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue Advanced Synthesis and Catalysis Année : 2021

Palladium‐Catalyzed Regioselective C−H Arylation of 4‐Azaindazole at C3, C5 and C7 Positions

Résumé

Direct and site-selective C5 and C7 palladiumcatalyzed C-H arylations of 4-azaindazole N-oxide have been achieved. A bidentate ligand and Pd(OAc)2 catalyst in toluene promoted the activation of C5 position, while a phosphine ligand and PdCl2 catalyst in DMA directed the arylation at C7 position. Using this new method, the synthesis of C5, C7-diarylated 4-azaindazole N-oxides as well as the C3, C5 C7 triarylated 4-azaindazoles was achieved towards future medicinal compound development.
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hal-03416452 , version 1 (05-11-2021)

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Soukaina Faarasse, Saïd El Kazzouli, Otmane Bourzikat, Stéphane Bourg, Samia Aci-Seche, et al.. Palladium‐Catalyzed Regioselective C−H Arylation of 4‐Azaindazole at C3, C5 and C7 Positions. Advanced Synthesis and Catalysis, 2021, 363 (16), pp.3937-3945. ⟨10.1002/adsc.202001421⟩. ⟨hal-03416452⟩
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