Development of a Reproducible and Scalable Method for the Synthesis of Biologically Active Pyrazolo[1,5-a]pyrimidine Derivatives

Abstract A reproducible and scalable method has been developed for the synthesis of a series 3,6-substituted pyrazolo[1,5- ]pyrimidines, which are basis rational design selective inhibitors AMP-activated protein kinase. Regarding formation new types carbon skeleton, applicability Suzuki–Miyaura cross-coupling using Buchwald ligands to form C–C bond in sterically hindered position 6 5,7-dimethyl-substituted ]pyrimidine shown.