Glycosylative coupling of 13 and 16 proceeded smoothly using AgOTf and NIS (Scheme 5). We had previously envisioned a Schmidt reaction between the trichloroacetimidate derivative of 11 and 16; while we were able to synthesize the trichloroacetimidate of 11, the product was very unstable and difficult to handle. The azide of 17 was converted into the corresponding amine using a Staudinger reduction. 18 was reacted with commercially available ethyl 2-ethoxy-2-iminoacetate in THF. We observed that the resulting amidine ethyl carboxylate was highly unstable and was partially hydrolyzing during the attachment step, affording a mixture of products which was difficult to separate. Quenching the reaction with H2O and stirring for a few hours gave desired amidine carboxylic acid 19 as a single product in a two-step, one-pot protocol. The Cbz and benzyl groups were removed by hydrogenolysis; here, using a 1:1 mixture of glacial acetic acid and H2O as the solvent was far superior to earlier attempts with MeOH. The acetonides were cleaved with 6 M aqueous HCl in 1,4-dioxane. The synthetic (+)-kasugamycin hydrochloride salt was found to be identical with a commercial sample in all respects (see Supporting Information for full details).