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    The C3 direct arylation of 1H-indazole and 1H-7-azaindazole has been a significant challenge due to the lack of the reactivity at this position. In this paper, we describe a mild and an efficient synthesis of new series of C3-aryled 1H-indazoles and C3-aryled 1H-7-azaindazoles via a C3 direct arylation using water as solvent. On water, PPh3 was effective as a ligand along with a lower charge of the catalyst Pd(OAc)2 (5 mol%) at 100 °C, leading to C3-aryled 1H-indazoles or C3-aryled 1H-7-azaindazoles in moderate to good yields.

    Citation

    Khadija Gambouz, Abdelmoula El Abbouchi, Sarah Nassiri, Franck Suzenet, Mostapha Bousmina, Mohamed Akssira, Gérald Guillaumet, Saïd El Kazzouli. On Water" Palladium Catalyzed Direct Arylation of 1H-Indazole and 1H-7-Azaindazole. Molecules (Basel, Switzerland). 2020 Jun 18;25(12)

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    PMID: 32570894

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