IVERMECTIN 5,4"-BIS[(ARYL)AMINO](THIOXO)ACETATES, METHOD FOR PRODUCTION THEREOF AND ANTIPARASITIC AGENTS BASED THEREON Russian patent published in 2018 - IPC C07D493/22 C07H17/08 A01N43/90 A61K31/335 

FIELD: chemistry.

SUBSTANCE: invention relates to the field of macrolide chemistry, namely to previously unknown compounds – 5,4''-bis[(aryl)amino](thioxo) acetates of ivermectin of the general formula I (1 a-j) having antiparasitic activity, as well as to the method for their preparation and antiparasitic agents based on them. Method is that the ivermectin of formula III is reacted with acid chloride in an organic solvent medium in the presence of an amine type catalyst, followed by isolation of produced 5,4''-bis(chloroacetyl)ivermectin and treatment with its pre-prepared solution of sulfur and amine in DMF. As the organic solvent, for example, methylene chloride or chloroform is used. As the amine type catalyst, for example, pyridine, 2,6-lutidine or triethylamine is used. To improve the solubility of sulfur and to create a homogeneous reaction medium, triethylamine is added to the previously prepared sulfur and amine solution in DMF. Invention also relates to antiparasitic agents based on compounds of general formula I. 1a-j R= , , , , , , , III.

EFFECT: technical result of the proposed invention consists in the preparation of new compounds of general formula I possessing high antiparasitic activity, allowing them to be used to create effective antiparasitic agents compatible with auxiliary substances ointments, which widens the range of anti-parasitic products that can be used for external use in the fight against parasites.

8 cl, 1 tbl, 11 ex