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A regioselective C7 bromination and C7 palladium-catalyzed Suzuki-Miyaura cross-coupling arylation of 4-substituted NH-free indazoles.


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.

SUBMITTER: Boujdi K 

PROVIDER: S-EPMC8694914 | biostudies-literature | 2021 Feb

REPOSITORIES: biostudies-literature

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A regioselective C7 bromination and C7 palladium-catalyzed Suzuki-Miyaura cross-coupling arylation of 4-substituted NH-free indazoles.

Boujdi Khalid K   El Brahmi Nabil N   Graton Jérôme J   Dubreuil Didier D   Collet Sylvain S   Mathé-Allainmat Monique M   Akssira Mohamed M   Lebreton Jacques J   El Kazzouli Saïd S  

RSC advances 20210210 12


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

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