| abstract |
Process for the preparation of peracetyloxazolines from peracetyl saccharides. The process involves reacting the starting material, a peracetyl saccharide, with a combination of reagents to directly produce the peracetyl oxazoline. This method can be used to activate oligosaccharides, an oligosaccharide containing a reducing GlcNAc at the end of the chain being activated by the formation of an oxazoline at this end of the chain, then coupled to a bifunctional spacer to give an oligosaccharide/spacer conjugate. Then, this conjugate is coupled to a protein, such as granulocyte colony stimulating factor or interferon-gamma, to give a neoglycoprotein conjugate. A method of forming neoglycoprotein conjugates capable of improving the biological and physiochemical characteristics of the protein has been provided. For example, serum shelf life or efficiency of peptide delivery to a target organ or target cell can be improved. |