METHOD FOR OBTAINING ALKYL-SUBSTITUTED 4-HALOGEN-3-HYDROXYFURO[3,4-c]PYRIDIN-1(3H)-ONES Russian patent published in 2016 - IPC C07D491/48 

FIELD: chemistry.

SUBSTANCE: invention relates to method of obtaining novel alkyl-substituted 4-halogen-3-hydroxyfuro[3,4-c]pyridin-1(3H)-ones of general formula I , wherein R¹=R²=CH₃, Hlg=Cl; R¹=CH₃, R²=C₂H₅, Hlg=Cl; R¹=CH₃, R²=C₃H₇, Hlg=Cl; R¹=R²=CH₃, Hlg=Br; R¹=CH₃, R²=C₂H₅, Hlg=Br; R¹=CH₃, R²=C₃H₇, Hlg=Br, which consists in the fact that respective 3-amino-8-hydroxy-1,6-dioxo-2,7-diazaspiro[4.4]non-3-en-4-carbonitryl is dissolved in 2-5-fold excess of concentrated hydrohalic acid, then 5-7-fold excess of phosphorus (III) halogenide is added, reaction mass is boiled for 40-50 minutes, cooled, diluted with water and extracted with ethylacetate. Extract is evaporated, formed sediment is re-crystallised from propan-2-ol. These compounds can find application as activator of potassium channels, inhibitors of anaplastic lymphoma kinase (Anaplastic Lymphoma Kinase), inhibitor of cholesteryl ether transfer protein (CETP), as well as cardioprotector agents.

EFFECT: increase of prime yield.

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