Protection of 3-propylxanthine (I) using p-methoxybenzyl chloride (II) afforded the 7-(p-methoxybenzyl) derivative (III), which was further alkylated at position 1 with butyl iodide and K2CO3 to give (IV). Finally, removal of the p-methoxybenzyl group of (IV) by means of H2SO4 in the presence of anisole in refluxing trifluoroacetic acid yielded the title xanthine.