METHOD FOR OBTAINING A NEW AMINO ACID-BASED DERIVATIVE AND AN ACETYLCHOLINESTERASE INHIBITOR (ACHE) BASED ON IT Russian patent published in 2022 - IPC C07C231/00 C07C237/22 A61K31/16 

FIELD: pharmaceutical chemistry.

SUBSTANCE: invention relates to the field of pharmaceutical chemistry, specifically to a method for obtaining an amino acid-based derivative characterized by formula (I) having inhibitory activity against acetylcholinesterase (AChE). The method involves the interaction of compounds characterized by the structural formulas (II), (III), (IV) and (V) in the presence of methanol, followed by treatment of the reaction mixture sequentially with chloroform and saturated NaHCO₃ solution. Further evaporation of the solvent and purification of the final product by flash chromatography using a mixture of dichloromethane solvents (DCM)/MeOH with a volume ratio of solvents of 30:1, which contains 0.1 wt.% NH₃, lead to the final product in the form of a syrup from pale yellow to white amorphous solid. In these formulas, R¹ is benzyl, n-propyl, R² is n-butyl, cyclohexyl, n =1, 2. The invention also relates to acetylcholinesterase (AChE) inhibitors obtained by this method, which have an increased effectiveness of inhibiting AChE.

EFFECT: expansion of the range of methods for obtaining amino acid-based derivatives.

2 cl, 42 dwg, 4 tbl, 4 ex