Ten derivatives of 3-(Substituted)Benzyl-7-but-2-ynyl-1-methyl-8-(4-methylenepiperidin-1-yl)-3,4,5,7-tetrahydro-purine-2,6-dione was efficiently synthesized from simple available starting materials using two-step. 8-Bromo-7-but-2-ynyl-1-methyl3,4,5,7-tetrahydro-purine-2,6-dione was reacted with 4-Methylene-piperidine using Buchwald-Hartwig approach to give intermediate 7-But-2-ynyl-1-methyl-8-(4methylene-piperidin-1-yl)-3,4,5,7-tetrahydro-purine-2,6-dione, formed intermediate was reacted with substituted benzyl bromides using potassium carbonate in microwave gives aimed compounds. Synthetic Buchwald-Hartwig methodology was found great importance for the synthesis of reported derivatives.