METHOD FOR PRODUCING AN ACETYLCHOLINESTERASE (AChE) INHIBITOR AND INHIBITOR PRODUCED BY THE METHOD Russian patent published in 2022 - IPC C07C231/00 C07C237/22 A61K31/16 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to the field of pharmaceutical chemistry and medicine production technology, specifically, to a method for producing acetylcholinesterase (AChE) inhibitors by the formula (VI). Method consists of two stages. At the first stage, a compound by the formula (I) is produced through the interaction of compounds characterised by structural formulas (II), (III), (IV), and (V), respectively, in the presence of methanol, followed by treating the reaction mixture consecutively with chloroform and a saturated NaHCO₃ solution, with subsequent evaporation of the solvent and purification of the end product by flash chromatography using a mixture of dichloromethane/MeON solvents at a 30:1 volume ratio of the solvents, containing 0.1% wt. NH₃, resulting in the end product in the form of a syrup of a pale yellow to white amorphous solid substance. At the second stage, a compound by the formula (VI) is produced through the interaction of compounds characterised by formulas (I) and (VII), respectively, wherein compound (I) is dissolved in acetone and methylated with dimethyl sulphate (1 eq.), resulting in a compound by the formula (VI) in the form of a pale yellow syrup. In the above formulas, R¹ constitutes benzyl, n-propyl; R² constitutes n-butyl, cyclohexyl; n = 1, 2. The invention also relates to an acetylcholinesterase (AChE) inhibitor produced by the method.

EFFECT: proposed method allows producing new acetylcholinesterase (AChE) inhibitors.

, ,

2 cl, 65 dwg, 6 tbl, 8 ex