METHOD FOR PRODUCING 7-SUBSTITUTED 4,4-DIMETHYL-9-OXO-4,4A-DIHYDRO-9H-XANTEN-2-CARBONIC ACIDS AND THEIR CYTOTOXIC ACTIVITY Russian patent published in 2018 - IPC C07D311/86 A61K31/352 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to the method for producing 7-substituted 4,4-dimethyl-9-oxo-4,4 and-dihydro-9H-xanten-2-carboxylic acids of the general formula (I) , where: R=CH₃O (Ia); R=CH₃ (Ib); R=H (Ic); R=Br (Id); R=CL (Ie), by reacting 6-substituted 3-(4-oxo-4H-chrome-3-yl) acrylic acids, where the substituents have the above values, with enamine N-(2-methylprop-1-enil) pyrrolidine at a temperature of 20 to 80°C for 0.5 to 4 hours in the presence of a catalyst of lanthanum nitrate (III) in an amount of 0 to 20 moll. % in a medium of the solvent selected from dichloromethane, ethyl acetate, or acetonitrile and N-(2-methylprop-1-enil) pyrrolidine is used in 10-100% excess, relative to acrylic acids, followed by crystallization of the target product upon acidification of the reaction mass.

EFFECT: reduction of process time, simplification of the technology of isolation of target compounds exhibiting a cytotoxic activity.

2 cl, 1 tbl, 6 ex