Development of a reproducible and scalable method for the synthesis of biologically active pyrazolo[1,5-<i>a</i>]pyrimidine derivatives

Abstract

A reproducible and scalable method for the synthesis was developed, and 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, was obtained and characterized. In the course of the formation of new types of carbon skeleton, the possibility of applying Suzuki-Miyaura cross-coupling with Buchwald ligands to form C-C bond in the sterically hindered position 6 of 5,7-dimethyl-substituted pyrazolo[1,5- a ]pyrimidine was shown.