ARYLATED POLYCARBOXYL FULLERENE DERIVATIVES, METHODS FOR PRODUCING THEM, COVALENT CONJUGATES, METHOD FOR PRODUCING THEM Russian patent published in 2015 - IPC C01B31/00 C07C57/40 C07C51/09 A61K31/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical and pharmaceutical industries, and concerns chemical functionalisation of fullerene C₆₀, particularly a method for organic fullerene [60] derivative synthesis, including soluble in water and physiological media. A problem of producing high-stable polycarboxyl fullerene C₆₀ derivatives applicable in biomedicine or pharmacology, as well as for producing fullerene derivative conjugates with other medicinal preparations is solved within the invention by creating a new class of arylated polycarboxyl fullerene C₆₀ derivatives containing aromatic carboxylic acid (carboxylic acid derivatives) fragments attached to a fullerene frame, as well as a method for producing these compounds. The invention defends structures and a method for producing a particular class of polycarboxyl arylated fullerene C₆₀ derivatives having a composition and structure described by general formula 1, namely . The invention also refers to a method for producing the compounds described by general formula 1, by means of conducting a reaction of fullerene C₆₀ halogen derivatives with protected derivatives of aromatic carboxylic acids in the presence of Lewis acids as a catalyst. The polycarboxyl compounds are further produced in the form of free acids by acid hydrolysis. .

EFFECT: invention can find application in biomedical investigations and manufacturing of new medicinal preparations applicable for therapy of human and animal diseases; more specifically, the invention refers to new arylated polycarboxyl fullerene C₆₀ derivatives and a method for producing them.

9 cl, 4 dwg, 2 tbl