Alchemia Pty Ltd

Gyula Dekany

Istvan Toth

Barry Kellam

John Papagerogiou

Laurent Francois Bornaghi

The invention provides collections of orthogonally-protected monosaccharides as universal building blocks for the synthesis of glycoconjugates of non-carbohydrate molecules, neo-glycoconjugates and oligosaccharides. This orthogonal protection strategy allows for the specific deprotection of any substituent ono the saccharide ring, and greatly facilitates targeted or library-focused carbohydrate-related syntheses. In particular, the invention provides a universal monosaccharide building block of General Formula (I) or General Formula (II) in which A is a leaving group; X is hydrogen, O, N or N; Xis hydrogen, &#x2014;CHO&#x2014;, &#x2014;CHNH&#x2014;, &#x2014;CH, &#x2014;CHNor &#x2014;COO&#x2014;; and B, C, D and E are protecting groups that can be cleaved orthogonally, and in which B, C, D and E are absent when X is hydrogen or N, and E is absent when Xis hydrogen, CHor N.

Protecting groups for carbohydrate synthesis

This invention relates to methods for synthesis of organic compounds, and in particular to compounds useful as protecting and linking groups for use in the synthesis of peptides, oligosaccharides, glycopeptides and glycolipids. The invention provides protecting and linking groups that are useful in both solid phase and solution synthesis, and are particularly applicable to combinatorial synthesis.

Protecting and linking groups for organic synthesis on solid supports

The invention provides a system for solid-phase synthesis of oligosaccharides, based on the discovery that a 2-substituted-1,3-dioxocycloalkyl linker group of general formula (I) can be used to couple saccharide groups of both the O-glycoside and N-glycoside type to a polymer support. The invention provides reagents, reagent kits and methods for solid-phase oligosaccharide synthesis.

Oligosaccharide synthesis

The invention provides amine-protecting groups for use in solution phase or solid-phase oligosaccharide synthesis, in which a 2-substituted 1,3-dioxo compound is used to protect one or more primary amine groups of an aminosugar or gylycosylamine. The invention provides reagents, reagent kits, and methods for solution phase, solid-phase oligosaccharide synthesis.

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Ruislip, United Kingdom

Gyula Dekany