METHOD OF PRODUCING WATER-SOLUBLE NON-AGGLOMERATIVE FULLERENE IMMUNOSTIMULATING NANOPARTICLE AND WATER-SOLUBLE NON-AGGLOMERATIVE FULLERENE IMMUNOSTIMULATING NANOPARTICLE Russian patent published in 2014 - IPC C07D295/15 B82B1/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a water-soluble non-agglomerative fullerene immunostimulating nanoparticle which consists of a hydrophobic fullerene core which is covalently bonded to a capronyl ligand through a piperazine spacer (1,2-dihydrofullerene-1-(6-piperazin-1-yl)-caproic acid) and a method for production thereof, which involves synthesis of pure 1,2- dihydrofullerene-1-(6-piperazin-1-yl)-caproic acid in four steps, the first of which involves obtaining 4-Boc-1-(5-ethoxycarbonyl-pentyl)-piperazine; the second step involves obtaining 6-(piperazin-1-yl)-caproic acid ethyl ether by dissolving 4-Boc-1-(5-ethoxycarbonyl-pentyl)-piperazine in 2N HCl and evaporating the obtained solution, pH of the precipitate of which is brought to a value of 10.0; extracting with ethyl acetate to dry the organic layer; the third step involves obtaining ethyl ether of 1,2- dihydrofullerene-1-(6-piperazin-1-yl)-caproic acid by mixing and stirring until dissolution of fullerene-C₆₀ and toluene with addition, after dissolution, of Cp₂TiCl₂ and ethyl ether of 6-(piperazin-1-yl)-caproic acid and subsequent elution with a mixture of hexane and chloroform mixture, and the purified 1,2- dihydrofullerene-1-(6-piperazin-1-yl)-caproic acid in form of the finished product is obtained by dissolving ethyl ether of 1,2-dihydrofullerene-1-(6-piperazin-1-yl)-caproic acid in ethyl alcohol with addition of NaOH solution and heating the mixture while stirring until complete homogenisation. The pH of the reaction mixture is then brought to a neutral value and the precipitated acid is separated by microfiltration on filters for subsequent washing off of nanoparticle residue and evaporation of the drain residue, which consists of the water-soluble non-agglomerative fullerene immunostimulating nanoparticles, consisting of a hydrophobic fullerene core which is covalently bonded to a capronyl ligand through a piperazine spacer.

EFFECT: improved method.

4 cl, 4 dwg, 1 tbl