Federalnoe gosudarstvennoe byudzhetnoe obrazovatelnoe uchrezhdenie vysshego obrazovaniya "Moskovskaya gosudarstvennaya akademiya veterinarnoj meditsiny i biotekhnologii - MVA imeni K.I. Skryabina (FGBOU VO MGAVMiB - MVA imeni K.I. Skryabina)
发明人:
Dzhafarov Mamed Khangusejnovich,Mirzaev Mikail Nurbagandovich,Vasilevich Fedor Ivanovich,Zavarzin Igor Viktorovich,Shchetinina Marina Anatolevna,Chernoburova Elena Ivanovna
申请号：
RU20170130507
公开号：
RU2670202(C1)
申请日:
2017.08.29
申请国别(地区):
俄罗斯
年份:
2018
代理人:
摘要：
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 ge
