METHOD OF SOLID-PHASE PEPTIDE SYNTHESIS Russian patent published in 1995 - IPC

FIELD: peptide chemistry. SUBSTANCE: method of solid-phase synthesis of peptides of the general formula (I) R₁-R₂-R₃-Ser-Tyr-R₄-heu-R₅-Pro-R₆, where R₁= nupo-Glu, N-Ac D Nal; R₂=His, Dp Cl Phe, Dp F Phe, R₃=Trp, D-Trp; R₄=D Nal(2); Dh Arg(Et)₂, Dh Arg(Bu), Dh Arg(CH₂CF₃)₂, R₅=Arg, L-Arg(Et)₂, L-hArg(Bu), L-hArg(CH₂CF₃)₂; R₆= GlyNH₂; DAla NH₂ involves addition of N-protected terminal amino acids to inert solid carrier followed by increment of N-protected amino acids to the joining peptide chain. Side chain of serine residue is protected temporarily with the group showing lability with relation to agents which were used for removal of alpha-aminoprotected groups. Side chain of histidine (if it is present) is protected with the group showing lability with relation to alpha-aminodeblocking agent. At the end of each cycle protected groups were removed, polypeptide is desplit from carrier, and aminolysis or ammonolysis is used, and synthesized compound of the formula (I). EFFECT: improved method of synthesis.