Abstract: Methods for producing amrubicin and structural analogs thereof. The present invention encompasses synthetic pathways for the production of amrubicin (Formula I) and structural analogs thereof. The synthetic pathways of the present invention preferably employ as a starting material an anthracycline compound having the generic Formula II: Compounds of Formula II may have any combination of the following identities for the indicated moieties: R1, R2, R3, R4, and R8 may be H, OH, or alkoxy; R5 may be H, alkyl, or alkoxycarbonyl; R6 may be H or alkyl; R7 may be OH or alkyl. In certain embodiments, ?-rhodomycinone or daunomycinone may be used as starting materials according to Formula II. The present invention employs a compound of Formula II as part of a semi-synthetic method that combines traditional chemical synthetic steps with biosynthetic steps to produce amrubicin, derivatives thereof, and structural analogs thereof.