Palladium-Catalyzed Synthesis of 5‑Iminopyrrolones through Isocyanide Double Insertion Reaction with Terminal Alkynes and Water

Abstract

With the combination of Pd­(dppf)­Cl2 and Cu­(OAc)2, a variety of 5-iminopyrrolones were synthesized in moderate to good yields from terminal alkynes, isocyanide, and water via isocyanide double insertion and cycloaddition reaction. A plausible reaction mechanism for this process is depicted. Furthermore, selected compounds 3c, 3e, and 3h exhibited good activities against HepG2 (human liver cancer), NCI-H460 (human lung cancer), and SK-OV-3 (human ovarian cancer) cell lines with IC50 values in the range of 10.63–22.63 μmol L–1

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The Francis Crick Institute

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Last time updated on 12/02/2018

This paper was published in The Francis Crick Institute.

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