An efficient synthesis of a variety of 1,2-disubstituted-5,6-dihydropyrrolo[2,1-α]isoquinoline derivatives via an acid-promoted cyclization reaction between 1,2,3,4-tetrahydroisoquinoline (THIQ) and substituted α,β-unsaturated aldehyde derivatives is reported. This cycloaddition allows access to structurally diverse multisubstituted dihydropyrrolo[2,1-α]isoquinolines in moderate to good yields, which was the core scaffold of marine natural alkaloid lamellarins.
© 2022 The Authors. Published by American Chemical Society.