METHOD OF SYNTHESIS OF SUBSTITUTED 1-AMINONAPHTHALENE-5-SULFAMIDES Russian patent published in 1995 - IPC

FIELD: organic chemistry. SUBSTANCE: products: substituted 1-aminonaphthalene-5-sulfamides, for example, compounds containing -NR₁R₂ in sulfamide group where it represents: a) N(CH₃)C₂H₅; b) -NH(CH₃); c) -NH(C₂H₅); d) -N-hexamethylene; e) ; f) . Synthesis is carried out by reaction of thionyl chloride with 1-nitronaphthalene-5-sulfoacid in the medium of dimethylformamide followed by amination of formed amine in the medium of organic solvent, CCl₄, CH₂Cl₂, benzene or in two-phased system: toluene or benzene aqueous solution of Na₂CO₃ and reduction of synthesized product, for example, in methanol medium in the presence of Raney nickel or by treatment with reducing agents Fe/HCl or SnCl₂/HCl/HCl. Under these conditions the pure end products can be produced useful for protease analysis indicated above. Method can be used in biochemistry for enzymatic activity of proteases. EFFECT: improved method of synthesis of substrates, decreased cost, simplified method. 2 cl, 2 tbl