PROCESS FOR COVALENT COUPLING FOR THE PRODUCTION OF CONJUGATES, AND PRODUCTS HEREBY OBTAINED

摘要

ABSTRACT.A process to produce by covalent binding con-jugates of a substance containing a 2-amino-2-deoxy-glycopyranosyl residue the NH2-function of which in itsmost stable conformation is equatorially oriented, and asubstrate containing a primary amino group. This is doneby subjecting the substance to degradation by diazo-tation to form a substance fragment having a freeterminal aldehydo group, said fragment through itsaldehydo group being reacted with the amino group ofthe substrate to form a Schiffs base which is then byreduction converted to a secondary amine.The substance is preferably selected from oligoand polysaccharides containing glucosamine or galactoseamine units. The substrate is suitably selected fromsurface-aminated plastic objects, aminated gels andproteins.The conjugate described consists of an 1-deoxy--2,5-anhydrohexitol unit which constitutes terminalunit in an oligo or polysaccharide and which in1-position is covalently bound to an amino groupassociated with a substrate.