Abstract: Thiazolopyrimidine scaffold is important pharmacophore in compounds which have shown various biological activities. The objective of this review is to compile the literature concerning existing approaches applied for these fused heterocycles construction with an emphasis on recent developments. This paper also reviews the current literature references with regard of prospects and challenges of condensed thiazolopyrimidine derivatives application for the directed synthesis of biologically active substances and analysis of recent advances in pharmacology screening of this heterocyclic compounds.