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Issue 38, 2016
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Total synthesis of diptoindonesin G and its analogues as selective modulators of estrogen receptors

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Abstract

We have developed a versatile synthetic strategy for the synthesis of the natural product diptoindonesin G and its analogues as selective modulators of estrogen receptors. The strategy involves a regioselective dehydrative cyclization of arylacetals, a regioselective bromination of benzofurans, a sequential cross-coupling of bromo-benzofurans with aryl boronic acids, and a BBr3-mediated tandem cyclization and demethylation. Preliminary biological studies uncovered the critical and dispensable phenolic hydroxyl groups in the natural product and also revealed unexpected selectivity for isoforms of estrogen receptor.

Graphical abstract: Total synthesis of diptoindonesin G and its analogues as selective modulators of estrogen receptors

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Publication details

The article was received on 01 Aug 2016, accepted on 05 Sep 2016 and first published on 12 Sep 2016


Article type: Communication
DOI: 10.1039/C6OB01657J
Citation: Org. Biomol. Chem., 2016,14, 8927-8930
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    Total synthesis of diptoindonesin G and its analogues as selective modulators of estrogen receptors

    J. Liu, T. J. Do, C. J. Simmons, J. C. Lynch, W. Gu, Z. Ma, W. Xu and W. Tang, Org. Biomol. Chem., 2016, 14, 8927
    DOI: 10.1039/C6OB01657J

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