Patent ID: 8063202

Claim:
A process for preparing glycopeptide having at least one asparagine-linked oligosaccharide at a desired position of the peptide chain thereof and a residue of sialic acid or a derivative thereof at a terminal and thereof, the process comprising: a. esterifying a hydroxyl group of a resin having the hydroxyl group and a carboxyl group of an amino acid having amino group nitrogen protected with a fat-soluble protective group, b. removing the fat-soluble protective group to form a free amino group, c. amidating the free amino group and a carboxyl group of an amino acid having amino group nitrogen protected with a fat-soluble protective group, d. removing the fat-soluble protective group to form a free amino group, e. repeating the steps c and d at least once, f. amidating the free amino group and a carboxyl group of the asparagine portion of an asparagine-linked oligosaccharide having amino group nitrogen protected with a fat-soluble protective group, g. removing the fat-soluble protective group to form a free amino group, h. amidating the free amino group and a carboxyl group of an amino acid having amino group nitrogen protected with a fat-soluble protective group, i. repeating the steps g and h at least once, j. removing the fat-soluble protective group to form a free amino group, k. cutting off the resin with an acid, and l. transferring fluoro-sialic acid to the resulting glycopeptide using a sialic acid transferase and CMP-7-fluoro-sialic acid, CMP-8-fluoro-sialic acid, or CMP-9-fluoro-sialic acid.