The present invention relates to an arbekacin synthesis method. According to the arbekacin synthesis method, di-tert-butyl
dicarbonate is adopted as a protection agent, tert-butyloxycarbonyl protection is performed on three amino groups on the sites C3, C2' and C6' of 3',4'-dideoxy-3',4' didehydro-
kanamycin B, difference between the remaining
free amino groups on the site 1 and the site 3' is adopted to directly and selectively introduce the
side chain on the amino group on the site 1, the amino-protected 1-tert-butoxy
amide-3-
hydroxybutyric acid is directly adopted as an
acylation reagent of the amino group on the site 1, and
hydrolysis with an acid is adopted to remove the tert-butyloxycarbonyl protection. According to the present invention, the operations of the method are simple, the reaction condition and the protection group removing condition are mild, the separation purification of the product obtained from the reaction is easy compared with the separation purification of the product obtained by adopting other types of the
amino acid protection agents, the one-pot reaction is adopted, the concurrent deprotection is adopted, the product yield is high, the production cost is reduced, the industrial production is easily achieved, and hydrazine
hydrate and other hazardous compounds are not used so as to provide the advantages of low environment
pollution.