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Metal-free directed C-H bond activation and borylation

Release time:2019-10-01    clicks:870

The group publishes a Metal-free directed C-H bond activation and borylation on Nature. Congrats Lv !

ABSTRACT: Organoboron reagents are important synthetic intermediates that play a key role in the construction of natural products,pharmaceuticals, and organic materials. The discovery of simpler, milder and more efficient approaches to organoboronsopens a route to diverse substances. Here we show a general method of directed C–H activation for site-selective C–Hborylation of arenes and heteroarenes avoiding the use of metal catalysts. C7 and C4-borylated indoles are produced bya mild approach with broad functional group compatibility. The mechanism involves BBr3 as both reagent and catalystand is established with DFT calculations. Downstream transformation of the formed boron species to natural productsand drug scaffolds highlights the potential utility of this strategy.