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A regioselective C7 bromination and C7 palladium-catalyzed Suzuki–Miyaura cross-coupling arylation of 4-substituted NH-free indazoles†
Nabil El Brahmi,Jérôme Graton,Didier Dubreuil,Sylvain Collet,Monique Mathé-Allainmat,Mohamed Akssira,Jacques Lebreton,Saïd El Kazzouli
RSC Advances Pub Date : 02/10/2021 00:00:00 , DOI:10.1039/D0RA08598G
Abstract

A direct and efficient regioselective C7-bromination of 4-substituted 1H-indazole has been achieved. Subsequently, a successful palladium-mediated Suzuki–Miyaura reaction of C7-bromo-4-substituted-1H-indazoles with boronic acids has been performed under optimized reaction conditions. A series of new C7 arylated 4-substituted 1H-indazoles was obtained in moderate to good yields.

Graphical abstract: A regioselective C7 bromination and C7 palladium-catalyzed Suzuki–Miyaura cross-coupling arylation of 4-substituted NH-free indazoles
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