AVERMECTIN B 5-O-HEMISUCCINATE AMIDES, METHOD FOR PRODUCTION THEREOF AND ANTI-PARASITIC 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, specifically to previously unknown compounds – avermectin B₁ hemisuccinate amides general formula I, R=a: NH-CH₂-C₆H₄ b: N(Et)₂ c: NHCH(CH₃)CH₂OCH₃ d: NH(CH₂)₅CH₃ e: NH(CH₂)₃CH₃ f: NH(CH₂)₆CH₃ g: NH(CH₂)₁₁CH₃

h: j:

having anti-parasitic activity, as well as a method for their preparation and an anti-parasitic agent based thereon. Method comprises reacting avermectin B₁ hemisuccinate of formula II with N-hydroxysuccinimide and N,N'-dicyclohexylcarbodiimide in an organic solvent medium, followed by treatment of the reaction mixture with an amine. Amine used is an aliphatic or aromatic amine or heteroaromatic amine. Organic solvent is preferably dimethylformamide. Process can be carried out at a temperature of 0 °C to room temperature. Invention also relates to anti-parasitic agents based on compounds of general formula I.

(II),

.

EFFECT: obtaining novel compounds of general formula I, having high anti-parasitic activity, which enables their use to produce effective anti-parasitic agents compatible with excipients of ointments, which widens the range of anti-parasitic products that can be used for external use in the fight against parasites.

6 cl, 1 tbl, 13 ex