Kasugamycin and minosaminomycin are structurally related aminoglycoside antibiotics (Figure ). Kasugamycin was first isolated in 1965 from a bacterial strain (Streptomyces kasugiensis) found in a soil sample near the Kasuga shrine in Nara, Japan. Shortly after isolation, empirical testing demonstrated that kasugamycin was active against a variety of bacteria and fungi. While its antibacterial activity is much less than that of other members of the aminoglycoside family, its ability to control rice blast disease caused by the fungus Pyricularia oryzae was so remarkable that it continues to be used commercially as an agricultural fungicide (Kasumin). Minosaminomycin is a structurally related antibiotic to kasugamycin and has demonstrable activity against a variety of pathogenic bacteria, including mycobacteria. Our interest in kasugamycin and minosaminomycin stems from both fundamental and applied considerations. These antibiotics have been synthetically unexamined for close to fifty years. Our laboratory has a deep interest in the development of new reactions which would enable the syntheses of complex antibiotics. Specifically, we envisioned that our laboratory's sulfamate-tethered aza-Wacker cyclization could serve as a key step for the assembly of the kasugamine portion of these antibiotics. Our interest in designing practical synthetic routes to antibiotics with new mechanisms of action relative to approved agents is motivated by the global rise in resistance to antibacterial and antifungal agents currently in use. It is our hope that de novo syntheses will allow for the rapid preparation of analogues and will serve as a start of a drug-discovery effort to replenish worrisome antibacterial and antifungal pipelines. In this account, we describe our preparation of a kasugamine synthon, a common building block for both kasugamycin and minosaminomycin.