The Journal of Organic Chemistry 2018-04-04

Intramolecular Aryne-Furan Cycloadditions for the Synthesis of Anticancer Naphthalimides

Sébastien Prévost, Ambre Dezaire, Alexandre Escargueil

Index: 10.1021/acs.joc.8b00531

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Abstract

An intramolecular aryne Diels–Alder reaction with a furan moiety was applied to the synthesis of dihydrobenzo[de]isochromenes as intermediates toward naphthalimides. After oxidation, this method offers an efficient approach for the synthesis of substituted naphthalimides, which showed potent cytotoxic activity against HT-29 human cancer cell line.