Catalytic Asymmetric Formal Aza-Diels-Alder Reactions of α,β-Unsaturated Ketones and 3H-Indoles

Asymmetric formal aza-Diels-Alder reactions with alpha,beta-unsaturated ketones and 3H-indoles with disubstituted groups on the C3 position catalyzed by primary amine-thiourea bifunctional catalyst have been developed. The reactions produced chiral hexahydropyrido-[1,2-a]indole-2-ones in high yields with excellent diastereo- and enantioselectivities.