Aaptamine, isolated from tropical marine sponges of the Demospongiae class, is the most prominent member of a growing family of natural products. Many aaptaminoids have been shown to have interesting biological activity. The efficient access to 5-methylaaptamine, an unnatural analogue of aaptamine, was achieved by using economic and naturally-occurring eugenol as the starting material. The synthesis involved the preparation of a 5-aminoeugenol derivative through successive nitration, O-methylation, and nitro group reduction reactions.