The invention relates to an
organic synthesis method, in particular to a method for synthesizing an Arbekacin and an intermediate dibekacin thereof. The method comprises the following steps of: takinga
kanamycin B as initial
raw material, carrying out the following processes of
aldol condensation, sulfonylation,
sodium iodide replacement and
elimination to form
double bond, de-protection under acidic condition, amino-
electron reduction and final hydrogenation, thus obtaining the dibekacin; taking 3',4'-dideoxy -3',4'-didehydro-
kanamycin B as
raw material, using a di-tert-butyl
dicarbonate toselectively protect the
amidogen of 3, 2', 6', 3'' sites; subsequently using the synthesized active ester to protect the 1-site
amidogen; subsequently using tri-
fluoroacetic acid to remove BOC; and carrying out hydrazinolysis and
catalysis and hydrogenation of
platinum oxide, thus obtaining the Arbekacin. The synthesis method has the advantages of simple operation, high outcome yield, reducing thecost of
raw material, optimizing the reaction
route, lowering the requirements to the
reaction conditions and being beneficial to industrial production.