Copper catalyzed arylation with boronic acids for the synthesis of N1-aryl purine nucleosides

The synthesis of a series of N1-aryl inosine and guanosine derivatives is described. The procedure for chemoselective N1-arylation involves the mild oxidative copper(II) mediated coupling with boronic acids. This approach provides access to substituted N1-aryl purines with interesting structural characteristics and novel scaffolds for drug discovery.