The invention discloses a synthesis and preparation process of an RGD cyclopeptide in the field of
solid-phase polypeptide synthesis. A new method comprises the steps as follows: a 2-
chlorine trityl chloride resin is selected and taken as a carrier;
D aspartic acid amino acid with a special protection group of a first side-chain carboxyl is grafted firstly; then a linear
peptide of an RGD sequence
peptide is grafted on the resin; after the last
amino acid is grafted, the protection group FMOC of the amino group is not required to be removed by using
piperidine, a special catalyst is added, and the side-chain carboxyl protection group of the first
D aspartic acid is removed from the resin directly; then
piperidine is added, and the amino protection group FMOC of the terminal
amino acid is removed; then a condensing agent is directly added to the resin, the carboxyl and the amino group which are exposed at the head end and the
tail end of the linear
peptide are subjected to
dehydration synthesis, so that the cyclopeptide is formed in an amido bond manner; and finally, the cyclopeptide is
cut down from the resin directly by using a
cutting liquid. The synthesis and preparation process of the RGD cyclopeptide has the advantages as follows: the process is advanced, the operation is simple, the product yield is high, the synthetic efficiency is improved, and the like.