Abstract 6-Formyl- and 6-hydroxymethyl-5,8-dihydroxy-2-methoxy-1,4-naphthoquinones were, respectively, prepared from 2-formyl- and 2-hydroxymethyl-1,4,5,6,8-pentamethoxynaphthalenes which were synthesized as key intermediates of the new antibiotics containing 2-methoxynaphthazarin structure.