PROESS FOR PREPARING 5-ARGINYLAMINONAPHTHALENE-1-SULPHAMIDES

Invention is intended for the improvement of arginyl derivatives containing aminonaphthalene sulfamides. Compounds described by the invention are used in biotechnology as chrome and fluorogenic substrates for establishing protease ferment activity using the new analysis method (ANSA). Material output makes only 35-40 percent, when they are produced by using known methods in rough conditions, when many intermediary stages and toxic materials such as dicyclohexylcarbodiimide are present and at the same time forming benzyl bromide as a by-product. The aim of the invention is to increase the output and simplify the process is achieved by the reduction of a number of stages, declining from use of hard to obtain toxic reagents, avoiding by-product formation. The process is executed: (N-nitro-N-tert butyloxycarbonyl)arginine is condensed in pyridine with 5-aminonaphthalene-1-sulfamide in dioxane at a presence of di-tert butylpyrocarbonate further using chromatography and cleaning the reaction mix up to a analytically pure product. N-nitro-N-tert butyloxycarbonyl groups are split off by hydrogen hydrogenation, in HCl methanol solution participating Pd/C as a catalyst. The produced di-hydrochloride is treated by NaHCO3. Output amounts to 64.8-79.4 percent.