AMIDES OF N-(2-AMINOPURIN-6-YL)-6-AMINOCAPROIC ACID, HAVING ANTI-TUMOUR ACTIVITY AND SYNTHESIS METHOD THEREOF Russian patent published in 2016 - IPC C07D473/16 A61P35/00 

FIELD: pharmaceutics.

SUBSTANCE: in general formula 1

(1a) R=Me, R'=H, X=O, Y=Z=F; (1b) R=H, R'=Me, X=O, Y=Z=F; (1c) R=Me, R'=H, X=CH₂, Y=Z=H; (1d) R=H, R'=Me, X=CH₂, Y=Z=H; (1e) R=Me, R'=H, X=CH₂, Y=Z=F; (1f) R=H, R'=Me, X=CH₂, Y=Z=F. Invention also relates to method of producing of N-(2-aminopurine-6-yl)-6-aminocaproic acid amides of general formula (1). Method involves acylation of corresponding enantiomerically pure chiral heterocyclic amines of general formula , where X, Y, Z, R, and R′ have values given above, with acyl chloride of 6-phthalimidecapronic acid, removal of phthaloyl protective group under action of hydrazine hydrate, nucleophilic substitution of obtained compounds with chlorine atoms in 2-acetamido-6-chloropurine followed by acetyl group alkaline hydrolysis in obtained product.

EFFECT: invention relates to N-(2-aminopurine-6-yl)-6-aminocaproic acid of general formula 1, which have high anticancer activity and low toxicity.

3 cl, 1 tbl, 6 ex