Dibekacin and arbekacin synthetic methods

摘要

The present invention also relates a method for the synthesis of dibekacin and arbekacin. This method, kanamycin B as the initial raw material, tert- butoxycarbonyl group is depending on to protect the five amino groups of the kanamycin B, to protect the hydroxy of aldol condensation is 4 "and 6" position, then 2 and 4 , 5 tri-containing imidazole, 3 'and 4' the position of the hydroxy and consumption divided by the presence of triphenylphosphine and imidazole to form an epoxy, and then delete said protection of the amino group and a hydroxy methanol solvent of hydrochloric acid, contact get the dibekacin hydrogenated. 3 ', 4'-deoxidation -3', 4'-dehydrogenation - kanamycin B as a raw material, all of the amino and hydroxy protected with a trimethylsilyl group, then the synthesized active ester is the 1-position of the an amino group carried out the acylation, using hydrochloric acid and hydrazine hydrate delete said protecting group according to the order, to get the arbekacin and finally catalytic hydrogenation. This synthetic method is operation easy, the yield is high and the environment friendly, production cost is low, which is advantageous for industrial production.