"On Water" Palladium Catalyzed Direct Arylation of 1H-Indazole and 1H-7-Azaindazole.
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.
['Gambouz|Khadija|K|', 'El Abbouchi|Abdelmoula|A|', 'Nassiri|Sarah|S|', 'Suzenet|Franck|F|', 'Bousmina|Mostapha|M|', 'Akssira|Mohamed|M|', 'Guillaumet|Gérald|G|', 'El Kazzouli|Saïd|S|0000-0001-5021-3571']
D002384:Catalysis D007191:Indazoles D010165:Palladium D014867:Water
arylation C–H functionalization azaindazole green chemistry indazole water.