In summary, we have completed the first enantioselective total syntheses of (+)-kasugamycin and (+)-kasuganobiosamine. The synthesis of (+)-kasugamycin proceeds in a longest linear sequence of 15 steps from a known epoxide and with an approximate yield of 12%. An intermediate in this sequence was used for the preparation of (+)-A highlight of our syntheses is our laboratory's sulfamate tethered reaction. This work underscores the power of tethered aza-Wacker chemistry for complex nitrogenous molecule assembly.