The invention discloses a method for increasing yield of
amikacin. The method for increasing yield of
amikacin comprises the following steps: heating, refluxing and carrying out reaction on gamma-amino-alpha-
hydroxybutyric acid and fluorenylmethyl
chloroformate, so as to generate a reaction liquid containing gamma-amino-alpha-
hydroxybutyric acid; directly adding N-hydroxyl
phthalimide and N,N-dicyclohexylcarbodiimide into the reaction liquid, and carrying out reaction to generate a reaction liquid containing active ester; directly adding a
kanamycin A
silanization compound into the reaction liquid containing the active ester for carrying out
acylation reaction, after complete reaction is finished, adding an HBr
aqueous solution until the pH is adjusted to be 2-3, and carrying out suction
filtration to remove
solid impurities; and then carrying out reduced pressure
distillation for removing the
solvent, adjusting the pH to be 7-8 with concentrated liquor, purifying by virtue of a CD180
macroporous resin column, concentrating, and carrying out
freeze drying, so that
amikacin solid is obtained. The active ester causes selectivity of the
acylation reaction to be greatly improved due to enlargement of a protective group, and a follow-up
processing step is also greatly simplified, so that the amikacin synthesis yield is increased.