Organocatalytic Enantioselective One‐Pot Four‐Component Ugi‐Type Multicomponent Reaction for the Synthesis of Epoxy‐tetrahydropyrrolo[3,4‐b]pyridin‐5‐ones

In the presence of a catalytic amount of chiral BINOL-derived phosphoric acid (TRIP), reaction of an α-isocyanoacetate 1, an aldehyde 2, an aniline 3 followed by addition of a toluene solution of α,β-unsaturated acyl chloride 5 afforded oxa-bridged tricycle 6 in excellent yield, diastereoselectivity and enantioselectivity. Six chemical bonds, five stereogenic centers, three cycles were formed in this one pot four-component reaction.