DOI: 10.3390/molecules31162827 ISSN: 1420-3049

Synthesis of Spiro-Bridged 3,4-Dihydrocoumarins Through an Organocatalytic Cascade Sequence Diels–Alder/Nucleophilic Ring Closing

Alberto Medina-Ortíz, José Luis Olivares-Romero, Alfonso Reyes-Luna, David Cruz Cruz, Clarisa Villegas Gómez

3,4-dihydrocoumarins and spiro compounds constitute an important class of privileged frameworks present in a wide variety of natural and synthetic molecules with diverse applications. In this study, we developed an organocatalytic methodology for the construction of complex and diverse chiral spiro-bridged 3,4-dihydrocoumarins through a Diels–Alder/Nucleophilic ring-closing cascade via trienamine activation. The reaction proceeds efficiently with different trienamine precursors and a range of coumarin-3-carboxamides, which act as both dienophile and intramolecular nucleophile species. This process affords the desired products in good yields and with a high degree of stereocontrol. Furthermore, several transformations on the newly formed spiro-piperidone ring demonstrate the synthetic utility of the obtained compounds.

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