Highly enantioselective organocatalytic synthesis of piperidines. Formal synthesis of (?)-Paroxetine

Valero, Guillem, Schimer, Jiri, Cisarova, Ivana, Vesely, Jan, Moyano, Albert and Rios, Ramon (2009) Highly enantioselective organocatalytic synthesis of piperidines. Formal synthesis of (?)-Paroxetine. Tetrahedron Letters, 50 (17), 1943-1946. (doi:10.1016/j.tetlet.2009.02.049).

Abstract

A highly enantioselective organocatalytic synthesis of piperidines is reported. The reaction is catalyzed by simple and commercially available secondary amines, affording the corresponding adducts with high yields and enantioselectivities. Moreover, this reaction is used for the formal synthesis of (?)-Paroxetine, a blockbuster drug, in only three steps.

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Contributors

Author: Ramon Rios

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