Process for the preparation of the mesylate salt trihydrate of 1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanol
AssigneePfizer Products Inc.
InventorsStanley Walter Walinsky, Terry Gene Sinay, Jr., Joseph Philip Rainville
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Abstract
The present invention is directed to a process for the preparation of the mesylate trihydrate of the (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanol compound having the formula (I): The present invention is also further comprises a process for enantiomeric resolution and isolation of the (D)-(−)-tartrate salt of the compound of the formula (I).
Claims12
A process forte preparation of the methanesulfonate trihydrate salt of a compound of formula (I):
- comprising the steps of
- (i) dissolving the D-(−)-tartrate salt of the compound of formula (I) in an aqueous methanesulfonic acid solution;
- and
- (ii) allowing the methanesulfonate trihydrate salt to separate out of solution.
A process for the preparation of the D-(−)-tartrate salt of a compound of formula (I):
- comprising the steps of
- (i) dissolving a racemic mixture comprising compounds of formulae (I) and (II)
- in an aqueous methanol solution having a water content of 5 to 20% in the presence of D-(−)-tartaric acid;
- and
- (ii) allowing the D-(−)-.tartrate salt of the compound of formula (I) to separate out of solution.
The D-(−)-tartrate salt of a compound of formula (I):
- wherein the ratio of the (1S,2S)-enantiomer to its (1R,2R)-antipode is greater than 97%.
Dependencies are inferred from the claim text.