The invention discloses an efficient
catalysis process for synthesis of
tildipirosin, and relates to the technical field of synthesis of
tildipirosin. The method comprises the following steps: dissolving
tylosin phosphate in
toluene, discharging the solution into a
reaction tube by a liquid pump, and discharging a
sodium borohydride /
methanol system into the
reaction tube from an upper
branch tube of the
reaction tube to obtain a
tylosin compound A; discharging the
tylosin compound A into a first reaction tank
system at a fixed flow rate, and discharging the tylosin
compound A into a first reaction tank one by one to obtain a tylosin compound B; discharging the tylosin compound B into a second reaction tank
system at a fixed flow rate, and discharging the tylosin compound B into a second reaction tank one by one to obtain a tylosin
compound C; and adding the tylosin
compound C into an
amination tank, adding
piperidine,
potassium carbonate and
acetonitrile to obtain a
tildipirosin crude product, and recrystallizing and refining the tildipirosin crude product. According to the method, the
aldehyde group at the C20 site of tylosin is oxidized into the hydroxyl group, so that only one
amination reaction is carried out later, and the problems of more byproducts, difficulty in separation, difficulty in reaction
controllability and the like in the conventional two
amination reactions are solved.