| 摘要 |
Invention is intended for an improved production method of arginyl derivatives containing various aminonaphthalene sulfamides. Afore mentioned compounds are applied in biotechnology as chrome and fluorogenic substrates for protease ferment activity determination using a new analysis method (ANSA). Obtaining substances by the known methods, harsh conditions are present, many intermediate stages are entered, including toxic reagents, such as dicyclohexylcarbodiimide, at the same moment forming by-product, benzyl bromide, the final output is up to 35-40 %. In order to increase the output and simplify the process itself, reduce number of intermediary stages, abandons the use of toxic reagents and forming by-products, the proposed process is performed by the condensing of N<α>-tert butyloxycarbonyl-arginine hydrochloride with 5-aminonaphthalene-1-penta-methylene-sulfamide (or other substituted amide) dimethylformamide and pyridine while present di-tert butyl pyrocarbonate and not extracting N<α> substituted product the reaction mix is affected by trifluorescence acid in methylene chloride and in NaHCO3 afterwards. The output is 62-84 %. |
