The domino Mannich/aza‐Michael reaction of γ‐malonate‐substituted α,β‐unsaturated esters with N‐protected arylaldimines has been achieved. Catalyzed by bifunctional thioureas, 2,5‐cis‐configured polysubstituted pyrrolidines are obtained in good to excellent yields (76–99%), enantioselectivities (75–94%) and excellent diastereoselectivities (de >95%). The pure stereoisomers are available by crystallization and removal of the racemates.
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Enders et al. (2010) studied this question.
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