Optically pure paroxetine precursors
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United States of America Patent
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Issued Date -
Jan 23, 2003
app pub date -
Jul 10, 2002
filing date -
Jul 13, 2001
priority date (Note) -
Abandoned
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Abstract
A biocatalytic process to obtain optically enriched derivatives of trans-4-(4-fluorophenyl)-3-hydroxymethylpiperidines, based on the enzymatic resolution of racemic precursors of formula III (where R.sup.3 is preferably phenyl or benzyl) by acylation of the hydroxyl group. Depending on the enzyme and the reaction conditions, either of the two enantiomers may be obtained with high enantiomeric purity. These compounds are important intermediates in the synthesis of the paroxetine anti-depressive agent. 1
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