PURPOSE:To obtain the titled substance useful for an antimicrobial agent against resistant microorganisms industrially and advantageously, by converting the groups at the 3'- and 2''-positions of a kanamycin A derivative having protected groups into imidazolylthiocarbonyl groups, deoxygenating the 3'-position of the reaction product with tributyltin hydride, and releasing the protected groups. CONSTITUTION:A kanamycin A derivative having protected groups of formula I (Ts is tosyl group) is reacted with thiocarbonylimidazole to introduce imidazolylthiocarbonyl groups into the hydroxyl groups at the 3'- and 2''-positions. The reaction product is then deoxygenated with tributyltin hydride to deoxygenate only the 3'-position selectively and give a reaction product of formula II. The resultant product is subjected to the removal of the imidazolylthiocarbonyl group from the 2''-position with aqueous ammonia, removal of the tosyl group with an alkali metal in liquid ammonia, ring opening of the 4',6'-carbamate ring through basic hydrolysis and removal of isopropylidene and cyclohexylidene groups through hydrolysis with an acid to give the aimed compound.
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