ASYMMETRIC SYNTHESIS OF DAPOXETINE OR DERIVATIVES THEREOF

摘要

PURPOSE: A method for preparing optically active compounds of dapoxetine or derivatives thereof is provided to conveniently prepare optically active compounds of dapoxetine or derivatives thereof in high yield and high optical activity while reducing reaction steps. CONSTITUTION: A method for preparing optically active compounds of dapoxetine or derivatives thereof includes: (i) reacting a compound of chemical formula 3 in the presence of oxidizing agent and organic rhodium metal catalyst and reacting the reactant with a compound of chemical formula 6 to prepare (S)-isomer of chemical formula 4a or (R)-isomer of chemical formula 4b; and (ii) reacting the product of (i) step with a compound of chemical formula 5, consecutively performing hydrolysis, reacting the hydrolysis reactant with a compound of chemical formula 7 or performing reduction amidation.