Industrial Chemical Synthesis of Modified Aminoglycoside Antibiotics

Abstract

On the basis of the mechanism of aminoglycoside antibiotic resistance, a number of semisynthetic derivatives of aminoglycoside antibiotics have been synthesized by deoxygenation and acylation. Among them, 3’, 4’-dideoxykanamycin B (Dibekacin) and 1-N-[(5)-4-amino-2-hydroxybutyryl] kanamycin A (Amikacin) have been commercialized and now widely used clinically. Dibekacin is demonstrated by our improvement on the industrial synthesis and Amikacin is reviewed from the view point of methodology of the selective acylation. © 1982, The Society of Synthetic Organic Chemistry, Japan. All rights reserved.