Abstract
An efficient synthesis of various N-substituted 3-aminoindazoles
using Buchwald-Hartwig C-N coupling reaction is
described. Several parameters were varied, including the nature
of the halogen atom and the protecting group of the starting materials,
as well as the effects of the catalyst system, base, solvent, and
reaction time. The efficiency of microwave versus conventional heating
was also compared to test the outcome of the reaction. Thus, by
applying this recent knowledge about metal-catalyzed aminations,
an alternative for the direct synthesis of primary 3-aminoindazoles
has been provided.
Key words
indazoles - amination - cross-coupling - palladium - copper - microwave promoted amination
