Process for the preparation of precursors acilados to - 3 - amino - 3 - desoxi alpha - D-glucopyranosyl (1 - amp; 6) - 6 - amino - 6 - desoxi alpha - D-glucopyranosyl - (1 - amp; 4) - n '- (4 - amino - 2 - hydroxy - 1 - oxobutil) - 2 - desoxi- D - estreptamina (amikacin)

摘要

Process for the preparation of a 3,6'-di-N-Acyl-1-[L-(-)-4-Acylamino-2-hydroxybutyryl] kanamycin A, wherein Acyl is a N-protecting acylating group, which comprises reacting kanamycin A with an aluminum salt in an inert organic solvent, treating the aluminum complex thus obtained with a N-acylating agent and acidifiying the reaction mixture, as such or after having removed the complexing aluminum in basic medium and isolated the 3,6'-di-N-Acyl-kanamycin A, to pH 6, treating the protonated 3,6'-di-N-Acyl-kanamycin A, in form of a salt thereof, with an active derivative of L-(-)-4-Acyl-amino-2-hydroxybutyric acid, wherein Acyl is a N-protecting group preferably identical with that which protects the amino groups in the positions 3 and 6' of kanamycin A, and isolating the product thus obtained by simple correction of the pH.