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Natural products

Taming reactive benzynes

Natural products often serve as sources of new drugs, either directly or after synthetic modification, but site-selective functionalization of complex small molecules is challenging. Now, a method has been developed that enables selective modification of a wide range of natural products by engaging a benzyne intermediate in a variety of reaction modes.

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Figure 1: Examples of the diverse reaction modes observed when complex natural products are reacted with a benzyne intermediate generated via a hexadehydro-Diels–Alder reaction.

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Correspondence to Paul J. Hergenrother.

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Tasker, S., Hergenrother, P. Taming reactive benzynes. Nature Chem 9, 504–506 (2017). https://doi.org/10.1038/nchem.2786

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