The invention discloses a synthetic method of 20,23-dipiperidine-5-O-carbomycin amine
glycosyl-
tildipirosin. The synthetic method comprises the following steps: (1) adding 20,23- dihalo-5-O-carbomycinamine
glycosyl-
tildipirosin,
piperidine and
potassium carbonate in a reaction container, carrying out heating refluxing for 4-5 h while stirring, after fluxing is finished, filtering an obtained mixing
system, adding
purified water in filtrate, fully stirring and then standing for layering, and separating to obtain an
organic layer; (2) adding pure water in the
organic layer again, adjusting pH value to be 2-3, standing for layering, separating to obtain a
water layer, cooling the
water layer to the temperature of 0 DEG C, adjusting pH value to be 8.0-8.5, standing for layering, separating toobtain a water phase, extracting the water phase by using an
organic solvent to obtain an organic phase, removing the
organic solvent, filtering, and concentrating till the product is dry to obtain acrude product; and (3) refining the crude product to obtain the 20,23-dipiperidyl-5-O-carbomycin amine
glycosyl-
tildipirosin. By the method, the 20,23- dihalo-5-O-carbomycin amine glycosyl-tildipirosin is directly used as a starting material, the
route for synthesizing tildipirosin is greatly simplified, and the synthesizing cost is reduced.