Carica papaya Lipase Catalysed Resolution of β??Amino Esters for the Highly Enantioselective Synthesis of (S)??Dapoxetine

P You, J Qiu, E Su, D Wei

Index: You, Pengyong; Qiu, Jian; Su, Erzheng; Wei, Dongzhi European Journal of Organic Chemistry, 2013 , # 3 p. 557 - 565

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Citation Number: 11

Abstract

Abstract An efficient synthesis of the (S)-3-amino-3-phenylpropanoic acid enantiomer has been achieved by Carica papaya lipase (CPL) catalysed enantioselective alcoholysis of the corresponding racemic N-protected 2, 2, 2-trifluoroethyl esters in an organic solvent. A high enantioselectivity (E> 200) was achieved by two strategies that involved engineering of the substrates and optimization of the reaction conditions. Based on the resolution of a series ...