The invention provides a synthesis process of
carbetocin. The synthesis process comprises the following steps: performing a
coupling reaction on Fmoc-Gly-OH with Rink
Amide-AM Resin obtained in the first step to obtain Fmoc-Gly-Rink
Amide-AM Resin; performing deprotection (20%
piperidine) with DBLK to obtain H-Gly-Rink
Amide-AM RFesin, and orderly completing the
coupling of the H-Gly-Rink Amide-AM Resin with Fmoc-Leu-OH, Fmoc-Pro-OH, Fmoc-Cys(Trt)-OH, Fmoc-Asn(Trt)-OH, Fmoc-Gln(Trt)-OH, Fmoc-Ile-OH, Fmoc-Tyr(Me)-OH and tetrachlorobutyric acid until
carbetocin linear
peptide resin is synthesized; mixing a
cracking agent with the
carbetocin linear
peptide resin obtained in the fourth step to have a
cracking reaction, thereby removing the Rink Amide-AM Resin and
side chain protecting groups; cyclizing the carbetocin linear crude
peptide into a carbetocin crude product, and separating and purifying the carbetocin crude product to obtain the carbetocin. The synthesis process has the advantages that the
polymerization side reaction is prevented, the process
route is greatly simplified, the production cost is reduced and the synthesis efficiency is improved; in addition, the purity of the finished product is high; in short, the synthesis process is convenient for large-scale production, and meanwhile, advantageous for
environmental protection, and has remarkable economic and
social benefits.