PYRIDONAMIDE PRODRUGS USED AS SODIUM CHANNELS MODULATORS Russian patent published in 2024 - IPC C07D213/18 C07F9/576 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a process of the preparation of a compound of formula I, in which independently for each case R² and R³ independently represent hydrogen, halogen or C₁-C₆-alkyl, where the specified C₁-C₆-alkyl is substituted by 0–6 halogen atoms; R⁵ is hydrogen, halogen, OH or C₁-C₆-alkyl, where the specified C₁-C₆-alkyl is substituted by 0–6 halogen atoms and where up to two non-adjacent CH₂ units of the specified C₁-C₆-alkyl can be replaced by -O-; R⁷ is hydrogen, halogen or C₁-C₆-alkyl, where the specified C₁-C₆-alkyl is substituted by 0–6 halogen atoms and where up to two non-adjacent CH₂ units of the specified C₁-C₆-alkyl can be replaced on -O-; and X is -PO(OH)₂, -PO(OH)O^-M⁺, -PO(O^-)₂⋅2M⁺ or –PO(O^-)₂⋅D2⁺; M⁺ is a pharmaceutically acceptable monovalent cation; and D²⁺ is a pharmaceutically acceptable divalent cation; provided that R², R³, R⁵ and R⁷ are not simultaneously hydrogen; comprising processing a compound of formula BK(PG₁)₂PO₄ to obtain a compound of formula C; and deprotection of the compound of formula C to give a compound of formula I wherein X is P(O)(OH)₂ and PG₁ is t-butyl; and optionally treating a compound of formula I in which X is P(O)(OH)₂, M⁺OH^- or D²⁺(OH^-)₂ to give a compound of formula I in which X is P(O)(OH)(O^-)·M⁺, P(O)(O^-)₂·2M⁺ or P(O)(O^-)₂·D²⁺. The invention also relates to compounds of formula B and formula C.

EFFECT: technical result is the preparation of compounds used as inhibitors of voltage-gated sodium channels.

28 cl, 5 dwg, 9 tbl, 19 ex