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Proline and its derivatives catalyze the asymmetric one-pot three-component aza-Diels–Alder reaction between unmodified α,β-unsaturated cyclic ketones, aqueous formaldehyde, and aryl amines with excellent chemo- and enantioselectivities (see scheme). Furthermore, this reaction provides a highly enantioselective entry to bicyclic non-proteogenic amino acid derivatives.
Sundén et al. (Thu,) studied this question.