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0.33g of the crude Boc-His (Boc) -Aib-OSu and 1g of the compound 2 obtained in example 2 were dissolved in 20mL of N, N-dimethylformamide, 2mL of N, N-diisopropylethylamine was added, the reaction was carried out at room temperature for 8h, ninhydrin was used to qualitatively detect the completion of the reaction, the result was positive, the reaction was continued for 24h, the result was negative, and a specific liquid phase diagram of the compound 4,1.08g, with a purity of 52.80%, was shown in FIG