FIELD: pharmaceutical industry.
SUBSTANCE: invention relates to a method for producing an antimicrobial peptidomimetic tripeptide of the formula H-Arg-Tbt-Arg-NH-C2H4-Ph by peptide synthesis in solution. The claimed method is characterized in that it includes the step of producing tert-butoxycarbonyl-L-arginine phenethylamide by the carbodiimide method, followed by deprotection of the tert-butoxycarbonyl group and obtaining phenethylamide-L-arginine dihydrochloride, obtaining a protected dipeptide - tert-butoxycarbonyl-2,5, 7-tri(tert-butyl)-tryptophanyl-arginine (2-phenylethyl)amide by the carbodiimide method, followed by removal of the tert-butoxycarbonyl group and obtaining dihydrochloride 2,5,7-tri(tert-butyl)-tryptophanyl-arginine (2-phenylethyl )amide, and obtaining a protected tripeptide - tert-butoxycarbonyl-L-arginyl-2,5,7-tri(tert-butyl)-tryptophanyl-arginine(2-phenylethyl)amide, followed by removal of the tert-butoxycarbonyl group, whereas at the stage of obtaining a protected dipeptide, an excess of 20 mole percent of phenethylamide-L-arginine dihydrochloride is used, and at the stage of obtaining a protected tripeptide, an excess of 20 mole percent of tert-butoxycarbonyl-L-arginine is used.
EFFECT: improved performance of tripeptide.
1 cl, 1 dwg, 1 ex
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Authors
Dates
2023-10-05—Published
2022-10-04—Filed