The one-step copper-mediated regioselective formation of the C8–S bond for purine derivatives with arylthiols was achieved using air as the green oxidant in the presence of 1.0 equiv of Na2CO3 and stoichiometric CuCl and 1,10-phenanthroline monohydrate. This method provides an economical, easy-to-handle, and effective method for the synthesis of 8-sulfenylpurine derivatives in moderate to excellent yields. The reaction is selective for C8 over C2 and C6. It also tolerates a free amine on the purine, and it has a wide substrate scope.

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A novel route to a wide range of 9-alkyl(benzyl)purin-8-one derivatives from purines reacting with (thio)ethers or methylarenes is described.

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