A method of making a derivatized aminoglycoside includes reacting an
aminoglycoside with at least 2 equivalents of a divalent metal ion in an
aprotic solvent to complex two neighboring amino group and hydroxyl group
pairs; reacting the non-complexed amino groups with a protecting reagent
to provide protecting groups; removing the divalent metal ion to provide
two unprotected amino groups; reacting one of the unprotected amino
groups with a reactive substance containing an linker, a carrier, or a
label; and removing the protecting groups. This method can be used to
produce novel compounds and reagents.