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Issue 53, 2017
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Rapid synthesis of bicyclic lactones via palladium-catalyzed aminocarbonylative lactonizations

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Abstract

A novel and efficient palladium-catalyzed aminocarbonylative lactonization of amino propargylic alcohols has been developed to provide rapid access to various bicyclic lactones especially dihydropyrrole-fused furanones, which are novel structures and have not been explored in biological and medicinal settings. This method can also be used to access β-lactone products such as 16. Preliminary biological evaluations revealed that compounds 13h and 13s demonstrated promising activity against Clostridium difficile and compounds 13h, 13k, 13s, and 16b showed activity against several important fungal pathogens.

Graphical abstract: Rapid synthesis of bicyclic lactones via palladium-catalyzed aminocarbonylative lactonizations

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Publication details

The article was received on 31 Mar 2017, accepted on 28 Apr 2017 and first published on 11 May 2017


Article type: Communication
DOI: 10.1039/C7CC02494K
Citation: Chem. Commun., 2017,53, 7238-7241
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    Rapid synthesis of bicyclic lactones via palladium-catalyzed aminocarbonylative lactonizations

    X. Yin, H. Mohammad, H. E. Eldesouky, A. Abdelkhalek, M. N. Seleem and M. Dai, Chem. Commun., 2017, 53, 7238
    DOI: 10.1039/C7CC02494K

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