Synthetic glycopeptides solid-phase synthesis

As a consequence of the progress and success of diverse oligomer libraries, experts in combinatorial synthetic oligomers, glycopeptide and oligosaccharide libraries, RNA-and DNA-aptamers have each contributed their news in these fields, while novel experimental examples of the use of templates in combinatorial chemistry for the solid-phase synthesis of multiple core structure libraries provide some insight to praxis-relevant work. 

As for peptides, yields obtained in solution synthesis of glycopeptides are often only modest and isolation of intermediates makes the approach cumbersome when performed on a small scale. Recent efforts have therefore mainly focused on solid phase synthesis, which today constitutes the most reliable and effident method for preparation of glycopeptides (12-15). Consequently, efficient synthetic routes to glycosylated amino adds are of central importance for the preparation of glycopeptides. 

SCHEME 11.2 Synthetic strategies of glycopeptides. (a) Convergent coupling, (b) solid-phase glycopeptide synthesis, and (c) enzymatic coupling. Asp, aspartic acid. 

This combination together with protecting groups such as Aloc,f l aUyl,f l and the Ddef groups, has widened the synthetic options considerably for sohd-phase peptide synthesis. This is now the method of choice for making most side-chain-modified peptides, for example phospho- and glycopeptides by solid-phase techniques. 

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