Efficient Synthesis of Pyrazolopyrimidine Libraries

摘要

The 1H-pyrazolo[3,4-d]pyrimidine ring system is an important structural template in anticancer research and in drug discovery as antibacterial1 and histamine release agents.2 There have been numerous recent literature reports on the synthesis of relatively small sets of compounds bearing the pyrazolopyrimidine core that have been shown to inhibit several oncogenic kinases including: GSK-3, mTOR, Src, AM, EGF-R, and PI3K. Because of the prevalence of this template in drug discovery, several reports of pyrazolopyrimidine library synthesis have also appeared.