Process for producing polyvalent and physiologically...

C - Chemistry – Metallurgy – 12 – P

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C12P 19/00 (2006.01) C07H 3/06 (2006.01) C12P 19/18 (2006.01) C12P 19/26 (2006.01) C12P 19/44 (2006.01)

Patent

CA 2192956

A process for preparing polyvalent and physiologically degradable carbohydrate receptor blockers by enzymatic glycosylation reactions and the use thereof for preparing carbohydrate building blocks The invention relates to a process for preparing polyvalent polymer-based carbohydrate receptor blockers which cause no intolerance reactions in vivo either in their entirety or in the form of degradation products. The carbohydrate side chain of the receptor blocker is assembled by enzymatic glycosylation reactions in aqueous buffer systems and homogeneous phase directly on the biodegradable polymer; the yields of the glycosylation reaction being considerably improved by comparison with the yields of known processes, as a rule taking place quantitatively and distinctly increasing the loading densities. Furthermore, a process for preparing the free oligosaccharides by means of the carbohydrate receptor blocker is prepared according to the invention is pro- posed.

L'invention concerne un procédé de fabrication de bêta-bloquants de glucides à base de polymère, ne provoquant, in vivo, ni dans leur totalité ni sous la forme de produits de décomposition, aucune réaction d'intolérance. La chaîne latérale glucide du bêta-bloquant est formée directement sur le polymère biodégradable au moyen de réactions de glycosylation enzymatique, dans des systèmes tampons aqueux et en phase homogène; les rendements de la réaction de glycosylation sont nettement supérieurs à ceux des procédés connus, se déroulent en général quantitativement et les densités d'accumulation sont nettement plus élevées. L'invention concerne en outre un procédé de fabrication d'oligosaccharides libres au moyen de bêta-bloquants de glucides obtenus selon le procédé mentionné ci-dessus.

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