Water-soluble coupling products - from active amino-cpds and carbonyl-polymers by solubilisation of residual carbonyl

摘要

Biologically active cpds. contg. amino-groups are converted into water-soluble products by coupling with polymers contg. carbonyl groups using part of the latter groups for coupling and modifying another for solubilisation. This is done by coupling with simple amino or sulphonic acids or as an after-treatment by a disproportionation or partial reducn. of the residual carbonyl groups. Products are soluble in a neutral-aq. medium and have a high content of active agent. In an example 3.1g (68%) product contg. 11% noradrenaline (twice the amt. obtainable without solubilisers) is obtd. from 1.1g glycine, 40 ml of a 10% oxydextran-soln. and 3.34 g noradrenaline bitartrate.