Journal of the American Chemical Society, Vol.129, No.23, 7256-7256, 2007
Asymmetric amine-intercepted nazarov cyclization
The chiral auxiliary directed addition of a propargyllithium reagent to a morpholino enamide, followed by exposure of the adduct to activated dry Florisil in the absence of solvent and in the presence of a primary or secondary amine, leads to a cascade of reactions that results in the formation of an aminocyclopentenone as a single diastereoisomer. The reaction can also be conducted intramolecularly.