PREPARATION OF ENZYMATICALLY STABLE COMPLEX GLYCOPEPTIDE

摘要

PROBLEM TO BE SOLVED: To obtain the subject enzymatically stable complex glycopeptide that can be expected to improve the stability and pharmaceutical action in situ and is useful for medicines by preparing a complex glycopeptide that is stable to an enzyme peptide: N-glycanase. SOLUTION: The objective compound is obtained by preparing a complex glycopeptide derivative that is stable to an enzyme peptide: N-glycanase (EC. 3. 5. 1. 52) preferably bearing a saccharide chain linking to the residual group of L-glutamine(Gln) in the peptide via the N-glycoside bond. The saccharide chain is introduced by using 9-fluorenylmethyloxycarbonyl-glutaminyl-N- acetylglucosaminide prepared by linking N-acetyl-D-glucosamine (GlcNAc) to Gin as a synthetic unit, to synthesize the glycopeptide to which GlcNAc is linked at the Gln residue through the solid phase method and by transfer-adding a saccharide chain to the resultant glycopeptide by using an enzyme: endo-β-N- acetylglucosaminidase.