Synthesis of 6,7,8-Trisubstituted Purines via a Copper-Catalyzed Amidation Reaction

We report herein an efficient method for the synthesis of 6,7,8-trisubstituted purines via a copper-catalyzed amidation reaction from easily accessible starting materials. Furthermore, the resulting 6-benzylsulfanyl-substituted purine derivatives may be readily oxidized for substitution by nucleophiles to give access to 6,7,8- trisubstituted purines for biological screening purposes.