AMINOCYCLOBUTANE DERIVATIVES, METHOD FOR PREPARING SAME AND USE THEREOF AS DRUGS Russian patent published in 2018 - IPC C07C235/40 C07C237/24 C07C255/57 C07D307/00 A61K31/165 A61P25/24 A61P29/02 A61P25/04 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: present invention relates to aminocyclobutane derivatives of general formula (1) or a pharmaceutically acceptable salt thereof, where X₁ represents a hydrogen atom or a fluorine atom; X₂ represents a hydrogen atom, or a fluorine atom, or a chlorine atom; R1 represents a hydrogen atom or a fluorine atom or a chlorine atom or a methyl group or a methoxy group or a cyano group; R2 is, independently or both, a methyl group or an ethyl group. Compounds of general formula (1) are obtained by reacting a secondary amine of formula (R2)₂NH with a compound of formula (C) to obtain a compound of formula (D), followed by converting the compound of formula (D) to an azide of formula (E), and then the azide group of the compound of formula (E) is reduced to the primary amine to obtain a compound of formula (1). Also, compounds of general formula (1) are obtained by converting a compound of formula (D) into an amine of formula (1) by Gabriel synthesis via an intermediate phthalimide of formula (F). Invention relates to intermediates of formula (D) or formula (C), where R1, R2, X₁ and X₂ are as defined for the compound of general formula (1). (1), (C), (D), (E), (F).

EFFECT: compound of formula (1) is intended for use as an NMDA receptor antagonist.

17 cl, 3 tbl, 1 dwg, 10 ex