Difluorination of α-(bromomethyl)styrenes <i>via</i> I(I)/I(III) catalysis: facile access to electrophilic linchpins for drug discovery

Joel Häfliger, Keith Livingstone, Constantin G. Daniliuc, Ryan Gilmour

Chemical Science · 2021 · 35 citations · 40 references

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Concepts

Abstract

difluorination to occur, thereby providing a platform to generate multiply fluorinated scaffolds for further downstream derivatization. The method facilitates access to a tetrafluorinated API candidate for the treatment of amyotrophic lateral sclerosis. Preliminary validation of an enantioselective process is disclosed to access α-phenyl-β-difluoro-γ-bromo/chloro esters.

References

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