METHOD OF SYNTHESIS OF (1S,2S)-1-(4-HYDROXYPHENYL)-2-(4-HYDROXY-4- PHENYLPIPERIDIN-1-YL)-1-PROPANOL METHANESULFONATE TRIHYDRATE AND D-(-)-TARTRATE SALT Russian patent published in 2003 - IPC

Abstract RU 2203888 C2

FIELD: organic chemistry, chemical technology. SUBSTANCE: invention relates to the improved method of synthesis of (1S,2S)-1-(4-hydroxyphenyl)-2-(4- hydroxy-4-phenylpiperidin-1-yl)-1- -propanol methanesulfonate trihydrate of the formula (I): that involves the following steps: (i) dissolving D-(-)-tartrate of compound of the formula (I) in methanesulfonate acid aqueous solution and (ii) isolation methanesulfonate trihydrate salt from solution. Method ensures to simplify process due to usage of D-(-)-tartrate salt of compound of the formula (I) as the parent substance instead free base of the formula (I) requiring additional step of its isolation and drying after separation of enantiomers. D-(- )-tartrate salt of compound of the formula (I) is prepared by dissolving racemic 1-(4-hydroxyphenyl)-2-(4- hydroxy-4-phenylpiperidin-1-yl)-1-propanol in aqueous methanol in the presence of D-(-)-tartaric acid and isolation of indicated salt from solution. EFFECT: improved method of synthesis and isolation. 11 cl, 2 tbl, 3 ex

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RU 2 203 888 C2

Authors

Rehjnvill Dzhozef Filip

Sinehj Terri Dzhin Ml.

Valinski Stehnli Uolter

Dates

2003-05-10—Published

2001-04-27—Filed