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
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Authors
Dates
2024-01-11—Published
2014-12-12—Filed