An enantioselective tandem sequence that comprises a cycloaromatization process followed by an intramolecular desymmetrizing Friedel‐Crafts alkylation of functionalized cyclohexadienones has been accomplished. The process takes place in good yields (65–95%), with excellent diastereoselectivity (>20:1) and enantiomeric ratios up to 90.5:9.5 in the presence of ( R )‐BINOL‐derived N ‐triflyl phosphoramides, and it gains access to a family of pyrrolo[2,1‐ a ]isoquinoline derivatives in a simple manner, with the simultaneous generation of two vicinal stereocenters, one of them a tetrasubstituted carbon stereocenter.
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Gaviña et al. (2024) studied this question.
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