METHOD FOR OBTAINING DERIVATIVES OF (2-HALOPYRIDINE-3,4-DIYL)DIMETHANOL Russian patent published in 2022 - IPC C07D213/30 C07D215/14 

FIELD: organic chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, and in particular to a method for obtaining derivatives of pyridine-3,4-diyldimethanol of general formula (1)

,

where X=Cl, R¹=R²=CH₃; X=Cl, R¹=CH₃, R²=C₂H₅; X=Cl, R¹+R²=(CH₂)₄; X=Br, R¹⁼R²=CH₃; X=I, R¹=R²=CH₃, which can be used as bioavailable inhibitors of PI3K5, activator of glutathione peroxidases, 5-hydroxytryptamine (5-HT₃) receptors, as antibacterial, antitumor agents, as well as substances used in the potential treatment or prevention of adenocarcinoma , sarcomas and heart failure. The proposed method includes the interaction of 5,6-disubstituted 2-halopyridine-3,4-dicarbonitrile with 80% sulfuric acid when heated to 150°C for 24-30 hours, the esterification of acid groups with methyl iodide in the presence of potassium carbonate and reduction intermediate obtained 5,6-disubstituted dimethyl 2-halopyridine-3,4-dicarboxylate with sodium borohydride in the presence of calcium chloride for 12-24 hours at room temperature, followed by purification of the obtained product by column chromatography.

EFFECT: development of a method for obtaining derivatives of pyridine-3,4-diyldimethanol with a yield of 62-79%.

1 cl, 5 ex