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

Abstract

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