This report demonstrates efficient formation of six-membered heterocycles using Michael-Aldol reactions, highlighting versatile use of dipolarophiles.
We report herein that alkenylpyridines could be used as dipolarophiles in the In/amine catalyzed cascade Michael-Aldol reactions with 3-furfurals, salicylaldehydes, and protected 2-aminobenzaldehydes, affording tetrahydrobenzofurans, 2H-chromenes and dihydroquinolines in good yields. This strategy features the activation of alkenylpyridine by InCl3 for the preparation of important six-membered heterocycles.
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Zhang et al. (2025) studied this question.
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