The invention relates to the field of
organic synthesis, in particular to a method for preparing Boc-His (Trt)-Aib-OH, which comprises the following steps: 1, adding 2-
aminoisobutyric acid, a
solvent and organic alkali into a reaction container, cooling, dropwise adding a
silicon protection
reagent, and heating for reaction after adding to obtain a 2-
aminoisobutyric acid solution protected by bis (trialkylsilyl); 2, dissolving Boc-His (Trt)-OH and an activating agent in a
solvent, dropwise adding a
coupling reagent, and after the reaction is finished, obtaining a Boc-His (Trt)-OH activated ester solution which is directly used for the next step; and step 3, cooling the Boc-His (Trt)-OH activated ester solution obtained in the step 2, dropwise adding the bis-trialkylsilyl protected 2-
aminoisobutyric acid solution obtained in the step 1, dropwise adding organic alkali after the dropwise adding is completed, slowly dropwise adding a
quenching reagent for
quenching after the reaction is completed, carrying out post-treatment on the reaction solution to obtain a Boc-His (Trt)-Aib-OH crude product, and
drying to obtain the Boc-His (Trt)-Aib-OH. And crystallizing the crude product to obtain a pure product of Boc-His (Trt)-Aib-OH. According to the method, purification of an intermediate is avoided, the reaction process is relatively well controlled, and high-quality Fmoc-Ser (tBu)-OH can be efficiently and stably prepared.