The invention relates to a
thymopentin methyl ester conjugate and a preparation method thereof. The preparation method specifically comprises the following steps: dissolving Z-FPSDM-Arg(Pbf)-Lys(BOC)-OH and 1-
hydroxybenzotriazole (HOBt) / DCC / MMF in
anhydrous trichloromethane, adding N,N-ethyldiisopropylamine and other specific solvents for reacting while stirring, thereby obtaining an active ester A; dripping the active ester into an alkaline solution of
tripeptide derivatives, adding N,N-
diisopropylamine and other specific solvents, thereby obtaining a coarse product of the
thymopentin methyl ester conjugate; and finally, performing deprotection, reduced pressure
distillation, washing and
drying, thereby obtaining an accurately modified
thymopentin methyl ester conjugate. The preparation method disclosed by the invention is fewer in byproducts and high in synthetic efficiency. The thymopentin methyl ester conjugate has the effects of maintaining the
biological activity of TP-5, relieving or avoiding enzymolysis of TP-5 and further obviously prolonging the in-vivo metabolic half-life, and is extremely high in clinical application value.