2-ARYL-1,3-THIAZOLIDINE-4-CARBOXYLIC ACIDS WITH ANTI-TUMOUR ACTIVITY Russian patent published in 2017 - IPC C07D417/12 C07D417/10 C07D277/06 A61P35/00 

FIELD: pharmacology.

SUBSTANCE: invention relates to 2-aryl-1,3-thiazolidine-4-carboxylic acids represented by general formula , wherein R¹ is -OR², -SR³, -NR⁴R⁵, where R² is an aryl moiety substituted at various positions with halogens, oxyalkyl groups; R³ is a condensed heterocyclic system selected from the group of benzothiazoles; -NR⁴R⁵ is substituted or unsubstituted heterocyclic systems in which the nitrogen atom is included into the saturated heterocycle selected from the group: 3,4-dihydroquinolines-2(H), pyrazoles substituted with methyl and nitro groups. The method for preparation of 2-aryl-1,3-thiazolidine-4-carboxylic acids with the general formula (I) is implemented by reacting 3-substituted anisaldehydes with cysteine in an alcoholic or hydroalcoholic medium, preferably 95% ethanol, at pH of 7-8 and at the boiling point of the reaction mass, followed by acylation of the resulting 2-aryl-1,3-thiazolidine-4-carboxylic acids with t-butylpyrocarbonate in a mixture of dioxane-water or dimethylformamide-water in the presence of a base. The product obtained is extracted with an organic solvent, the solvent is distilled off, the desired product is dried and isolated.

EFFECT: compounds have antitumor activity, and can be used to treat cancer.

2 cl, 1 tbl, 13 ex