PEPTIDE DERIVATIVES AND METHOD OF THEIR PRODUCTION Russian patent published in 1997 - IPC

FIELD: medicine, biology, particular, methods of peptide derivatives production. SUBSTANCE: product - derivatives of peptides of formula l: A-Ile-Y-Phe-B, where A-H, HVal, HSer- X-Val, Glp-Pro-Pro-Gly-Gly-Ser-X-Val; B - OH, Arg-OH; X - Lys, Arg; Y - Leu, Tie. Reagent 1: C-terminal amino acid. Reaction conditions: (1) successive building up of peptide groups with the help of activated esters protected by alpha-amino group of amino acids to obtain compounds of formula 1, where A -H, HVal, HSer-X-Val, which are subjected to fragmentary condensation in the presence of decyclohexylcarbonylimide and precluding racenization of additive with N-terminal compound: Glp-Pro-Pro-Gly-Gly-Ser-X-Val; (2) production of peptide derivatives of the formula: A-Ile-Y-Phe-OH, where A - Glp-Pro-Pro-Gly-Gly-Ser-X-Val is carried out by successive building up of group, beginning from C-terminal fragment up to obtaining N-terminal pentapeptide: Glp-Pro-Pro-Gly-Gly, dipeptide Ser-Arg and C- terminal tetrapeptide: Val-Ile-Leu-Phe, with condition of condensation of obtained fragments by successive attachment to above-mentioned N-terminal pentapeptide of dipeptide Set-Arg with the help of decyclohexylcarbonylimide in the presence of additive precluding racemization and attachment to obtained hexapeptide Glp-Pro-Pro-Gly-Gly-Ser-Arg of C-terminal tetrapeptide Val-Ile-Leu-Phe with the help of diphenylphosphoryazide. EFFECT: higher efficiency. 13 tbl