We report an efficient and practical strategy for the enantioselective synthesis of medicinally relevant hexahydroimidazo[1,2-a]quinolines via a copper(I)-catalyzed domino ring-opening cyclization (DROC) enabled by dynamic kinetic resolution (DKR) of racemic aziridines. The method affords the desired products in good to excellent yields (up to 88%), with outstanding diastereoselectivity (up to >99:1 dr) and high enantioselectivity (up to 94:6 er).
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Sharma et al. (2026) studied this question.
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