The invention discloses a preparation method of DOTATATE. The method comprises the following specific steps of: sequentially
coupling solid-phase carrier resin to amino acids, the N ends and side chains of which have protecting groups, according to the
amino acid sequence of DOTATATE, and then,
coupling DOTA(tBu)<3> so as to obtain linear
peptide resin of DOTATATE; then, adding
lysis solution to remove the protecting groups and
cutting the resin to obtain linear
peptide of DOTATATE; and finally, performing oxidization by using an
oxidizing agent to obtain DOTATATE crude
peptide. According to the preparation method in the invention, hydroxyl resin with easily available raw materials and low-price amino acids with
side chain protection are adopted to synthesize the linear peptide resin; then, the linear peptide is cracked; the
oxidizing agent easy to control is adopted to oxidize the linear peptide so as to obtain the target crude peptide; use of a highly toxic
reagent is avoided; and finally, purification, salt conversion, concentration and
drying are carried out, so that refined peptide is obtained. The method in the invention has the advantages of short synthesis
route, easily controlled linear peptide quality, low synthesis cost, high yield and high finished product purity, and is suitable for large-scale production.