METHOD OF SYNTHESIS OF delta-SLEEP PEPTIDE

摘要

FIELD: chemistry of peptides, medicinal chemistry. SUBSTANCE: method relates to the improved method of synthesis of delta-sleep peptide: Trp-Ala-Gly-Gly-Asp-Ala-Ser-Gly-Glu (I). Method involves condensation of pentafluorophenyl ester of Boc-protected tetrapeptide Boc-Trp-Ala-Gly-Gly-OPfp (II) c pentapeptide Asp-Ala-Ser-(X)-Gly-Glu (III) where X - acetyl or formyl in dimethylformamide in the presence of N-methylmorpholine followed by removal of Boc-group with formic acid at (-2)-(+8) C and acetyl or formyl group at alkaline condition and purification of the end product by chromatography. delta-Sleep peptide shows homogeneity (by TLC data), yield is 65-80%. EFFECT: improved method of synthesis, broad spectrum of physiological activity. 2 tbl, 1 dwga