Process for covalent coupling for the production of conjugates,

Details Process for covalent coupling for the production of conjugates, Process for covalent coupling for the production of conjugates,

1983-02-08

1986-09-23

Brown, Johnnie R.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

525 542, 536 21, 536 551, 536 553, C08B 3708, C08B 3710

Patent

active

046136657

ABSTRACT:
A process to produce by covalent binding conjugates of a substance containing a 2-amino-2-deoxyglycopyranosyl residue the NH.sub.2 -function of which in its most stable conformation is equatorially oriented, and a substrate containing a primary amino group. This is done by subjecting the substance to degradation by diazotation to form a substance fragment having a free terminal aldehydo group, said fragment through its aldehydo group being reacted with the amino group of the substrate to form a Schiffs base which is then by reduction converted to a secondary amine.
The substance is preferably selected from oligo and polysaccharides containing glucosamine or galactose amine units. The substrate is suitably selected from surface-aminated plastic objects, aminated gels and proteins.
The conjugate described consists of a 1-deoxy-2,5-anhydrohexitol unit which constitutes terminal unit in an oligo or polysaccharide and which in 1-position is covalently bound to an amino group associated with a substrate.

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