STEREOSELECTIVE PREPARATION OF 3-HYDROXY-3-PHENYLPROPIONITRILE

摘要

This invention relates to a Chemoenzymatic process for the stereoselective preparation of both (R) and (S) enantiomers of 3-hydroxy-3-phenylpropanenitrile, useful as a key intermediate for synthesis of (S)-fluoxetine, (R)-tomoxetine and cognant compounds, which comprises reacting cyanohydrin with an acetylating agent in the presence of lipase in an organic solvent, followed by separation of (R)-acetate and (S) alcohol, hydrolyzing (R)-acetate in presence K2CO3 in methanol, filtering the reaction mixture and evaporating the solvent to obtain the (R) alcohol.