The invention provides a preparation method of
dipeptide-2, which comprises the following specific steps: carrying out amino protection on L-
valine by using 2-(
trimethylsilyl) ethoxycarbonyl, carrying out
condensation reaction on the product and L-
tryptophan benzyl ester, carrying out deprotection to remove the 2-(
trimethylsilyl) ethoxycarbonyl, removing benzyl under a
palladium-carbon hydrogenation condition, and purifying to obtain the
dipeptide-2. Belongs to the technical field of
organic synthesis. According to the method, 2-(
trimethylsilyl) ethoxycarbonyl is adopted as an
amino acid protecting group, amino groups can be accurately and specifically protected, the operation steps of protecting the amino acids are simplified, conditions are simple to control and easy to implement, meanwhile, a
dipeptide intermediate is generated through a
condensation reaction, and a good product foundation is laid for subsequent preparation steps of dipeptide-2; in addition, the process reaction is rapid, the operation steps are simple and clear, the used reagents are easy to purchase and low in price, the method is very suitable for industrial large-scale production, and a new synthesis way is provided for preparation of the dipeptide-2.