INDUSTRIAL METHOD FOR PRODUCTION OF HIGH PURITY ESTETROL Russian patent published in 2023 - IPC C07J1/00 C07J75/00 A61K31/565 A61P15/00 A61P15/02 A61P15/12 A61P15/18 A61P17/00 A61P17/02 A61P25/00 A61P35/00 A61P37/00 A61P37/06 A61P5/30 

FIELD: chemistry.

SUBSTANCE: production of esthetrol having formula (I) starting from a compound having formula (II). The method is characterized in that (a) a compound having formula (II) is subjected to acylation in a suitable solvent with a suitable reagent, resulting in a compound having the general formula (III). Then (b) the benzyl protecting group at position 3 is removed by hydrogen transfer hydrogenation or catalytic hydrogenation, whereby a compound having the general formula (IV) is obtained. Then (c) the protection is removed in an alkaline medium formed by an alkali metal carbonate, an alkali metal hydrogen carbonate or alkali metal hydroxides in a suitable solvent. In formulas (III) and (IV), R represents a methyl group or a hydrogen atom. The proposed method allows to obtain high purity esthetrol. The invention also relates to compounds having the general formula (III) and (IV) which are used in said method.

EFFECT: new process.

19 cl, 5 ex