The present disclosure provides a method for the synthesis of IB-MECA. More specifically, the present disclosure provides a simple and high yield method for Good Manufacturing Production (GMP) of IB-MECA. The method involves the reaction of 6-halopurine-9-riboside with a diol protecting reagent； oxidation of the primary alcohol in the diol protected 6-halopurine-9-riboside with a diol protecting reagent； oxidation of the primary alcohol in the diol protected 6-halopurine； reaction of the diol protected 6-halopurine with a nucleophile (e.g. methylamine)； substitution of the halogen group with iodobenzylamine and removal of the diol protecting group.
