Hoechst Aktiengesellschaft

Hans-Ullrich Hoppe

Merten Schlingmann

Susanne Grabley

Axel Walch

Walter Dursch

Hans P Kraemer

Joachim Thiem

Hartmut Voelskow

Michael Magerstadt

Hubert Bader

Matthias Wiesner

Dieter Ulschneider

A cofactor having an aromatic or benzylic amino group is converted into an isothiocyanate by reaction with a compound such as thiophosgene and the isothiocyanate of the cofactor is attached to a polymer which is preferably water-soluble. When the polymer has amino groups, a thiourea bridge is formed between the polymer and cofactor and a polymer having hydroxyl groups results in a thiocarbamate bridge. The polymer may be a copolymer of vinylamine or vinylmethylamine and vinylmethylacetamide, partially alkylamine-substituted .alpha., .beta.-poly-(2-hydroxyethyl)-D,L-aspartamide, polyethyleneimine or carbohydrate. The cofactor bound to a polymer and an enzyme are contained in microcapsules or in a membrane to form an enzyme reactor.

Immobilization of an isethiacyanate of a cofactor on a polymer

Streptazoline is reacted with naphthoquinones in a Diels-Alder reaction, and the adduct is then oxidized. The resulting compounds have cytotoxic activity, in particular against leukemia cells, and have an antimicrobial action and act against protozoa.

Diels-alder adduct from streptazoline and naphthoquinones and its

In the process for the preparation of 4-benzyl aspartate starting from dibenzyl aspartate and/or its salts only one benzyl group is selectively removed by catalytic hydrogenation. By setting up appropriate reaction conditions elimination takes place mainly of the benzyl group on the C.sub.1 atom of the compound. The desired product can be isolated from the reaction mixture by precipitation.

Process for the preparation of 4-benzyl aspartate

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Hans-Ullrich Hoppe