Abstract An efficient palladium-catalyzed synthesis of 3-arylpyrazolo [1, 5-a] pyrimidines has been investigated. The key step in the synthesis is a Suzuki biaryl coupling of 3-bromo-2, 5- dimethyl-7-aminopyrazolo [1, 5-a] pyrimidines with arylboronic acids to provide 3- arylpyrazolo [1, 5-a] pyrimidines in moderate to good yield. The synthetic utility of this methodology has been demonstrated by a concise and convergent synthesis of R121920, ...