Purine derivatives are widely studied due to their biological activity and extensive potential in medicine. Thiopurine based compounds have already been proven as effective tools in the treatment of cancer and autoimmune disorders. A new synthetic approach for the synthesis of 6-azido-2-arylthiopurine derivatives 2 was developed. Further CuAAC reaction leaded to 6‑triazolyl-derivatives 3 with excellent yields. Additionally, by rearranging the synthetic approach regioisomers 6 were obtained.