METHOD FOR PREPARING PAROXETINE

摘要

PURPOSE: A method for preparing paroxetine is provided, thereby requiring no additional separation of cis and trans isomers, and preparing an enantiomeric excess of paroxetine using a small amount of catalyst and substrate under mild condition. CONSTITUTION: The method for preparing paroxetine represented by formula (I) comprises the steps of: (a) hydrogenating a compound of formula (III) using transition and chiral diphosphinic ligand as catalyst to prepare 4R-enantiomeric excess of compound of formula (IV); (b) racemization of the compound of formula (IV) under strong base to prepare 4R-trans compound of formula (V), and reacting the compound of formula (V) with a reducing agent to prepare a compound of formula (VI); (c) reacting the compound of formula (VI) with a reagent to convert -OH of compound of formula (VI) into a leaving group, nucleus-affinity substitution of the -OH converted compound with sesamol (3,4-methylenedioxyphenol) to prepare 4R-enantiomeric excess of derivatives of formula (VII); and (d) N-dealkylation of the compound of formula (VII), wherein R and R1 are selected from (C1-C5)alkyl, (C1-C5)carboxyalkyl, optionally substituted phenyl and optionally substituted benzyl.