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Synthesis of antidepressant duloxetine via asymmetric transfer hydrogenation
Authors:Shan Zhen He  Xue Ming Li  Jia Dai  Ming Yan
Affiliation:a The Industrial Institute of Fine Chemicals and Synthetic Drugs, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510080, China;b Guangdong Provincial People's Hospital, Guangzhou 510060, China
Abstract:
Antidepressant duloxetine (1) was prepared via asymmetric transfer hydrogenation of 3-(dimethylamino)-1-(thiophen-2-yl)propan-1-one (3). The Ru(Ⅱ), Rh(Ⅲ) and Ir(Ⅲ) complexes of several chiral ligands were examined as the catalyst and(S,S)-N-tosyl-1,2-diphenyl ethylenediamine (TsDPEN)-Ru(Ⅱ) complex was found to provide good yield and excellent enantios-electivity.
Keywords:Duloxetine  Synthesis  Asymmetric transfer hydrogenation
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