A one-pot process for the microwave-assisted synthesis of 7-substituted pyrazolo[1,5-a]pyrimidine

Abstract

An efficient synthesis of 7-substituted pyrazolo[1,5-a]pyrimidines using a one-pot, two-step process via Pd-catalyzed direct CH-arylation followed by a saponification–decarboxylation reaction is reported. Compared to the classical method (Negishi coupling), this new procedure has the advantages of convenient manipulation, short reaction times, excellent yields and the use of commercially available and relatively non-toxic compounds.