The silyl-protected 2'-amino-2'-deoxyadenosine (I) was acylated with 3-methoxybenzoyl chloride (II) to give the corresponding amide (III). Alkylation of (III) at N1 with 2-methylbenzyl bromide (IV), with subsequent Dimroth rearrangement using isopropyl amine in MeOH provided the N6-(2-methylbenzyl)adenosine derivative (V). Finally, fluoride-promoted desilylation of (V) in MeOH furnished the title compound.