Intermediate for synthesizing paroxetine, method for preparing the same, and uses thereof
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United States of America Patent
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Oct 24, 2017
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Jun 15, 2015
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Sep 22, 2014
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Abstract
A paroxetine intermediate, a method for preparing the same, and uses thereof are provided. Specifically, the method includes: reacting a compound of formula I below with a compound of formula II in the presence of an organic base under the catalysis of a complex formed from a chiral amine oxide L and a rare-earth metal compound Ln(OTf)3 to prepare a compound of formula III below: wherein R1 is alkyl, phenyl or benzyl; R2, R3, R4 are each independently C1-C6 alkyl or C6-C10 aryl; the chiral amine oxide L has the following structure: wherein n=1, 2; and R=Ph—, 2,6—Me2C6H3—, 2,6—Et2C6H3—, 2,6-iPr2C6H3—, Ph2CH—.
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