The palladium‐catalyzed direct C–H arylation of various heterocyclic is now recognized to be the most effective methodology for making aromatic compounds. In this paper, we present a new approach to control the site‐selective direct C–H arylation of both sp2 and sp3 sites in 5,7‐dimethyl‐2‐phenylpyrazolo[1,5‐a]pyrimidine by using aryl bromides. The desired compounds were obtained in satisfactory yields. The effects of each reaction parameter including catalyst, base, and solvent were investigated.
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