Process for the preparation of 4-(des-dimethylamino)-tetracyclines

摘要

The present invention refers to a process for the preparation of 4-(des-dimethylamino)-tetracyclines, which compounds have a therapeutical application. The starting tetracyclines are treated with a methylating agent and the resulting trimethylammonium salts are reduced by electrolysis in an aqueous solution at acidic pH, in the presence of an adequate electrolyte. A direct electrical current with a potential of 0.5-1.5 volts is applied between two convenient electrodes until the reaction is complete. The 4-(des-dimethylamino)-tetracyclines are isolated by extraction with an organic solvent.