Direct C−H Arylation of Purines: Development of Methodology and Its Use in Regioselective Synthesis of 2,6,8-Trisubstituted Purines

Direct C−H arylation of purines to position 8 by diverse aryl iodides was achieved with Pd catalysis in the presence of CuI and Cs2CO3. The
methodology is general and efficient and was applied in the consecutive regioselective synthesis of 2,6,8-trisubstituted purines bearing three
different C-substituents in combination with two cross-coupling reactions.