A direct entry to substituted piperidinones from α,β-unsaturated amides by means of aza double Michael reaction

Abstract

An intermolecular aza-double Michael reaction has been developed leading to functionalized piperidin-2-ones from simple starting materials. The method allows to utilize α,β-unsaturated amides as a synthon of piperidine nucleus. The short synthesis of anti-depressant paroxetine was demonstrated by using the new methodology.