This method demonstrates efficient synthesis of 2-hydroxy-1,2-dihydropyridines using iron(III), suggesting broader applications in organic synthesis.
An iron(III)-catalyzed methanesulfonic-acid-mediated [3 + 2 + 1C] annulation of enaminones assembling a 1,2-dihydropyridine (1,2-DHP) scaffold has been developed for the first time. This approach facilitates the rapid synthesis of 2-hydroxy-1,2-DHP derivatives in moderate to excellent yields with a broad substrate scope under mild conditions. The employment of 1,3-dioxolane as both a 1C synthon and solvent enables simultaneous incorporation of both a carbon atom and a hydroxy group into 1,2-DHPs. Application potential of this protocol is proven by its gram-scale preparation and further derivatizations.
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Hu et al. (2025) studied this question.
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