Demonstrates a new multicomponent reaction producing bicyclic lactols in drug synthesis, suggesting valuable synthetic pathways.
Herein, we introduce Morita–Baylis–Hillman-type yne-allylic esters that serve as novel precursors in a chemodivergent multicomponent reaction platform with carbon-based nucleophiles. SN2″ addition of tertiary amines generates unprecedented vinyl–allenyl ammonium intermediates, whose reactivity is substrate controlled. 1,3-Dicarbonyls afford linear dienol esters via an ABC-type multicomponent reaction (MCR), while aroylacetonitriles trigger a tandem [5 + 1] annulation to give bicyclic lactols. This work provides both a new MCR for drug conjugate synthesis and an efficient route to natural product-like bicyclic lactol scaffolds.
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Huang et al. (2026) studied this question.
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