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1.
Nature ; 575(7782): 336-340, 2019 11.
Artigo em Inglês | MEDLINE | ID: mdl-31723273

RESUMO

Organoboron reagents are important synthetic intermediates that have a key role in the construction of natural products, pharmaceuticals and organic materials1. The discovery of simpler, milder and more efficient approaches to organoborons can open additional routes to diverse substances2-5. Here we show a general method for the directed C-H borylation of arenes and heteroarenes without the use of metal catalysts. C7- and C4-borylated indoles are produced by a mild approach that is compatible with a broad range of functional groups. The mechanism, which is established by density functional theory calculations, involves BBr3 acting as both a reagent and a catalyst. The potential utility of this strategy is highlighted by the downstream transformation of the formed boron species into natural products and drug scaffolds.


Assuntos
Compostos de Boro/química , Compostos de Boro/síntese química , Boro/química , Produtos Biológicos/síntese química , Produtos Biológicos/química , Teoria da Densidade Funcional , Descoberta de Drogas , Indóis/química , Compostos Organometálicos/química , Preparações Farmacêuticas/síntese química , Preparações Farmacêuticas/química
2.
Nature ; 2019 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-31569198

RESUMO

Organoboron reagents are important synthetic intermediates that play a key role in the construction of natural products, pharmaceuticals, and organic materials.1 The discovery of simpler, milder and more efficient approaches to organoborons opens a route to diverse substances.2-5 Here we show a general method of directed C-H activation for site-selective C-H borylation of arenes and heteroarenes avoiding the use of metal catalysts. C7 and C4-borylated indoles are produced by a mild approach with broad functional group compatibility. The mechanism involves BBr3 as both reagent and catalyst and is established with DFT calculations. Downstream transformation of the formed boron species to natural products and drug scaffolds highlights the potential utility of this strategy.

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