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Selective C–H dithiocarbamation of arenes and antifungal activity evaluation

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Abstract

This paper discloses a transition metal-free selective C–H dithiocarbamation of drug skeletons using disulfiram (DSF) in the presence of KI/K2S2O8 in DMF/H2O. Drug skeletons, including 5-aminopyrazoles, indoles, pyrroloquinoline, and Julolidine, underwent C–H dithiocarbamation smoothly to afford a variety of drug-like molecules in moderate to good yields. It was found that the in situ formed 5-aminopyrazole iodide is the key intermediate for the dithiocarbamation. Bioassay results show that some of these N-heterocyclic dithiocarbamate derivatives exhibit good antifungal activity against Colletotrichum gloeosprioides and Fusarium oxysporum, F. proliferatum, Fusarium solani, Geotrichum candidum, Penicillium digitatum, Penicillium italicum, Phyricularia grisea.

Graphical abstract: Selective C–H dithiocarbamation of arenes and antifungal activity evaluation

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Article information


Submitted
23 Nov 2019
Accepted
24 Jan 2020
First published
25 Jan 2020

Org. Biomol. Chem., 2020, Advance Article
Article type
Paper

Selective C–H dithiocarbamation of arenes and antifungal activity evaluation

Z. Huang, X. Xia, Z. Huang, L. Xu, X. Zhang and R. Tang, Org. Biomol. Chem., 2020, Advance Article , DOI: 10.1039/C9OB02514F

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