METHOD OF OBTAINING DISPIROINDOLINONES Russian patent published in 2019 - IPC C07D487/20 

FIELD: chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, in particular, to a method for producing dispiroindolinones of general formula 1, where X is S or O; R1 is selected from the group comprising hydrogen, phenyl, phenyl, substituted by 1-2 substituents selected from halogen atom (fluorine, chlorine, bromine), hydroxy, lower alkoxy group (methoxy, ethoxy, isopropyloxy, propargyloxy) or C1-C6 alkyl (methyl, ethyl, propyl, butyl, pentyl, hexyl); R2 is selected from the group consisting of unsubstituted pyridyl or phenyl, substituted by 1-2 substituents selected from halogen atom (fluorine, chlorine, bromine), hydroxy, lower alkoxy group (methoxy, ethoxy, isopropyloxy, propargyloxy), aldehyde group or C1-C6 alkyl (methyl, ethyl, propyl, butyl, pentyl, hexyl); R3 is selected from the group consisting of a halogen atom, hydrogen atom or a nitro group; R4 is C1-C5 alkyl (methyl, ethyl, propyl, butyl, pentyl); R5 represents a hydrogen atom or alkyl C1-C3 (methyl, ethyl, propyl), characterized in that 1±0.1 molar eq. of the corresponding imidazolidin-4-one is dissolved in a monohydric alcohol, taken in an amount of 10 ml per 0.5±0.1 mmol, and boiled at 100±10 °C for 10±2 min after boiling the resulting solution, then sarcosine, taken at the rate of 2±0.2 eq., is added to the boiling mixture, and the corresponding isatin, taken in an amount of 2±0.2 eq. in relation to the corresponding imidazolidin-4-one, the resulting mixture is boiled until the end of the reaction, then the mixture is cooled to room temperature, the precipitated precipitate is filtered under vacuum with a glass porous filter and a Bunsen flask. 1.

EFFECT: new method has been developed for the preparation of dihydro derivatives based on 5-arylidene-2-thioxo-imidazolin-4-ones and 5-arylidene-2-oxo-imidazolidin-4-ones, which allows to obtain compounds with high yields.

1 cl, 1 tbl, 33 ex