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A mild two-step propargylation of aromatic bioactive small molecules

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Abstract

A two-step method for introducing a propargyl group in aromatic bioactive small molecules has been developed. This method features propargylation of aromatic groups using a cationic propargyl hexacarbonyl complex in the presence of cesium carbonate, and decomplexation of the resultant cobalt complexes using 2,2,6,6-tetramethylpiperidine-1-oxoammonium tetrafluoroborate. These reactions proceed under mild conditions, and thus are applicable for acid- and/or oxidant-sensitive aromatic bioactive small molecules.

Graphical abstract: A mild two-step propargylation of aromatic bioactive small molecules

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Publication details

The article was received on 30 Jun 2017, accepted on 08 Aug 2017 and first published on 08 Aug 2017


Article type: Paper
DOI: 10.1039/C7OB01587A
Citation: Org. Biomol. Chem., 2017, Advance Article
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    A mild two-step propargylation of aromatic bioactive small molecules

    N. Kanoh, T. Okamura, T. Suzuki and Y. Iwabuchi, Org. Biomol. Chem., 2017, Advance Article , DOI: 10.1039/C7OB01587A

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