METHOD FOR OBTAINING GLICLAZIDE Russian patent published in 2021 - IPC C07D209/52 

FIELD: drugs.

SUBSTANCE: invention relates to the field of drugs, more specifically to a method for producing gliclazide (N-(4-methylphenylsulfonyl)-N'-(3-azabicyclo[3.3.0]oct-3-yl)urea). The described method for obtaining gliclazide includes the interaction of tosyl chloride with an alkali metal cyanate in the presence of a heterocyclic amine in an anhydrous solvent at room temperature in an atmosphere of inert gas or in air without moisture, followed by the introduction of 3-amino-3-azabicyclo[3.3.0]octane into the resulting reaction mixture in the form of a free base or its hydrochloride, with or without the use of an inorganic salt additive in the reaction, and treatment of the contents of the reactor with acid and water at the end of the reaction, followed by isolation and purification of the target product. Sodium or potassium cyanate is used as the alkali metal cyanate. Derivatives of pyridine or quinoline are used as the heterocyclic amine.

EFFECT: reducing the staging of the production process to one stage; elimination of the need to comply with special industrial safety measures by eliminating the use of hazardous, toxic and unstable starting compounds and intermediates and carrying out synthesis under conditions that do not require the use of elevated temperature and pressure, corrosive environments and, in addition, obtaining a high quality product with a yield of up to 89%.

8 cl, 15 ex