Pyrazolopyrimidines: old molecules, new targets

Description

The synthetic strategies so far developed to build the pyrazolo[3,4-d]pyrimidine ring system and to generate highly functionalized analogs, with a particular emphasis on the 4-amino derivs., has been reviewed (75 refs.). The evolution of this versatile scaffold, starting from the pioneering work of Robins up to the recent prepn. of selective inhibitors (active against EGFR, Src, adenosine receptor etc.) has been discussed in terms of synthetic methodologies applied to the generation of more selective inhibitors. Being the literature on pyrazolo[3,4-d]pyrimidines particularly rich, the focus of this review deals with the construction of this ring system from pyrazoles only.

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